Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm degarelix cas 214766-78-6 hauv Suav teb. Txais tos rau kev lag luam wholesale zoo degarelix cas 214766-78-6 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Degarelixyog ib yam tshuaj, ib yam dawb los yog yuav luag dawb. Molecular formula C82H103ClN18O16, CAS 214766-78-6, molecular hnyav 1632.45 g/mol. Nws yog peptide compound tsim los ntawm ntau cov amino acid residues. Nws muaj cov tseem ceeb leucine residue saw, nrog rau ntxiv cov amino acid residues thiab lwm pab pawg tshuaj. Nws yog GnRH receptor antagonist uas txo cov qib testosterone los ntawm inhibiting qhov tso tawm ntawm gonadotropins nyob rau hauv anterior pituitary hlwb, yog li inhibiting kev loj hlob ntawm prostate qog. Kev nqus dej hauv lub cev yog nrawm, thiab cov tshuaj tau dav dav hauv cov ntaub so ntswg. Nws yog metabolized los ntawm daim siab thiab tso tawm los ntawm ob lub raum nyob rau hauv ob qho tib si metabolized thiab unmetabolized daim ntawv.
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Customized Bottle Caps Thiab Corks:
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Degarelix COA
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| Certificate of Analysis | ||
| Compound npe | Degarelix | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 214766-78-6 | |
| Ntau | 15g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202512090051 | |
| MFG | Peb 9, 2025 | |
| EXP | Peb 8 Dec 2028 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.43% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.54% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.9% |
| Ib leeg impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 90 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500 ppm |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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Tshuaj Formula |
C82H103ClN18O16 |
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Exact Mass |
1631 |
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Molecular Luj |
1632 |
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m/z |
1631 (100.0%), 1632 (88.7%), 1633 (38.8%), 1633 (32.0%), 1634 (28.3%), 1635 (12.4%), 1634 (10.4%), 1632 (6.6%), 1633 (5.9%), 1636 (3.6%), 1633 (3.3%), 1634 (2.9%), 1634 (2.6%), 1634 (2.1%), 1635 (2.0%), 1635 (1.9%), 1635 (1.3%), 1632 (1.1%), 1635 (1.1%), 1633 (1.0%) |
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Elemental Analysis |
C, 60,34; H, 6,36; Cl, 2,17; N, 15.45; 15.68 Nws |
Degarelixyog ib qho hluavtaws gonadotropin- tso tawm cov tshuaj hormone (GnRH) receptor antagonist, uas yog tus thib peb tiam ntawm cov tshuaj tiv thaiv androgen kho. Txij li thaum nws thawj qhov kev pom zoo hauv xyoo 2008, nws daim ntawv thov hauv kev kho mob qog noj ntshav prostate tau maj mam nthuav dav thiab ua kom pom qhov zoo ntawm cov tshuaj pharmacological. Nov yog nws cov ncauj lus kom ntxaws siv:
Lub mechanism ntawm kev txiav txim ntawm Degarelix: ncaj qha thaiv thiab ceev txo ntawm testosterone
Physiological hauv paus ntawm GnRH signaling pathway
GnRH yog secreted los ntawm lub hypothalamus thiab ua rau GnRH receptor nyob rau hauv lub anterior pituitary caj pas los ntawm pulsatile tso, stimulating lub synthesis thiab secretion ntawm follicle stimulating hormone (FSH) thiab luteinizing hormone (LH). Hauv cov txiv neej, LH ua haujlwm ntawm cov qog nqaij hlav hauv nruab nrog cev, txhawb cov synthesis ntawm testosterone (T); FSH ua haujlwm sib koom ua ke nrog testosterone los tswj cov phev ntau lawm. Testosterone yog lub ntsiab "roj" rau kev loj hlob ntawm cov qog nqaij hlav qog nqaij hlav prostate, thiab nws cov qib siab ua kom cov qog nqaij hlav.
Kev txwv ntawm tsoos GnRH agonists
Thawj tiam ntawm cov tshuaj tiv thaiv androgen (xws li leuprorelin thiab goserelin) yog GnRH agonists, thiab lawv cov teebmeem yuav tsum tau mus txog "thawj lub sijhawm stimulation": thaum pib siv tshuaj, GnRH receptors yuav qhib luv luv, ua rau muaj kev nce ntxiv hauv FSH / LH thiab testosterone theem ("flare spinional phenomenon"). tso zis tso quav thiab lwm yam mob qog nqaij hlav, tshwj xeeb tshaj yog nyob rau hauv cov neeg mob uas mob cancer prostate.
Direct antagonistic nyhuv ntawm Degarelix
Degarelix sib tw khi rau pituitary GnRH receptors, ncaj qha thaiv GnRH signaling yam tsis tas yuav tsum tau pib stimulation. Nws cov yam ntxwv muaj xws li:
Kev txo qis testosterone sai: Tom qab ib qho kev txhaj tshuaj, qib testosterone txo qis hauv 24 teev thiab tuaj yeem ncav cuag qib castration (<0.5 ng/mL) within 72 hours, which is more rapid than GnRH agonists (which take 2-4 weeks).
Kev tiv thaiv tsis tu ncua: Kev tuav tus neeg txais neeg nyob los ntawm ntev - kev npaj ua haujlwm (xws li kev txhaj tshuaj subcutaneous ib hlis ib zaug) txhawm rau inhibit testosterone secretion rau lub sijhawm ntev.
Tsis muaj qhov tshwm sim tshwm sim: Tsis txhob ua rau cov tsos mob hnyav tshwm sim los ntawm kev hloov pauv hormonal, tshwj xeeb tshaj yog haum rau cov neeg mob nyob rau theem siab lossis muaj cov tsos mob pom tseeb.
Degarelix lub ntsiab lus qhia: tag nrho lub voj voog tswj kev mob qog noj ntshav prostate
Kev kho mob thawj zaug hauv zos mob qog noj ntshav prostate
Applicable scenarios: High risk locally advanced prostate cancer (such as T3-T4 stage, Gleason score ≥ 8, PSA>20 ng / mL) yuav tsum tau txo qis ntawm testosterone theem los tswj cov qog loj hlob. Npaj kom tau txais radical prostatectomy los yog kev kho neoadjuvant ua ntej siv xov tooj cua kom txo cov qog ntim thiab txo qis pathological.
Cov ntaub ntawv pov thawj kho mob: Ib qho randomized tswj kev sim (RCT) tau pom tias pawg Degarelix muaj qhov zoo dua tom qab ua haujlwm pathological ua tiav cov lus teb (pCR) thiab cov paj tau zoo tshaj li pawg GnRH agonist, qhia tias muaj kev tiv thaiv ntxov ntxov dua -cov nyhuv qog.
Kev ua raws li lub sijhawm ntev- tau pom tias Degarelix tuaj yeem txo qhov kev pheej hmoo ntawm biochemical recurrence (BCR), tshwj xeeb tshaj yog rau cov hluas, cov neeg mob qog noj ntshav siab.
Kev sib xyaw ua ke rau metastatic castration resistant prostate cancer (mCRPC)
Kev ua haujlwm ua haujlwm: Hauv mCRPC theem, txawm hais tias testosterone tau mus txog qib castration, cov qog txuas ntxiv mus ntxiv los ntawm androgen receptor (AR) qhia txoj hauv kev. Degarelix txhim kho cov tshuaj tiv thaiv- qog ua haujlwm los ntawm kev cuam tshuam cov synthesis ntawm residual testosterone thiab adrenal androgens (xws li dehydroepiandrosterone, DHEA).
Kev sib xyaw ua ke: Siv ua ke nrog AR antagonists xws li enzalutamide, aparamide, thiab lwm yam, kom ncua kev vam meej tsis muaj sia nyob (PFS) los ntawm ob npaug thaiv AR signaling.
Ua ke nrog cov kws khomob: Docetaxel + Megarelix tuaj yeem cuam tshuam cov qog loj hlob thiab txhim kho lub neej zoo (QoL).
Ua ke nrog PARP inhibitors: Degarelix txhim kho DNA kev puas tsuaj kho inhibition los ntawm kev txo cov theem androgen hauv BRCA mutant mCRPC.
Intermittent androgen deprivation therapy (IADT) rau prostate cancer
Lub tswv yim kho mob: IADT tso cai rau kev rov ua kom luv luv ntawm qib testosterone los ntawm kev ncua tshuaj tiv thaiv androgen kom txo tau cov kev mob tshwm sim xws li pob txha thiab cov kab mob metabolic uas tshwm sim los ntawm ntev - lub sij hawm castration, thaum tswj kev tiv thaiv - cov qog nqaij hlav.
Qhov zoo ntawm Degarelix:
Kev rov qab sai ntawm testosterone: Tom qab txiav tawm, qib testosterone tuaj yeem rov qab los li qub hauv 1-2 lub lis piam, uas yog qhov zoo rau kev tswj lub voj voog ntawm IADT dua li GnRH agonists (uas siv sijhawm ntau lub hlis).
Txo qhov kev pheej hmoo ntawm kev cuam tshuam kev kho mob: zam kev mob qog nqaij hlav los ntawm kev rov qab qeeb tom qab GnRH agonist discontinuation.
Daim ntawv thov Degarelix hauv Kev Tsim Cov Tshuaj Hormone-Cov Qauv Kab Mob
Raws li kev xaiv gonadotropin ntau heev - tso cov tshuaj hormone (GnRH) receptor antagonist,Degarelixtuaj yeem ceev thiab tsis tu ncua inhibit qhov tso tawm ntawm luteinizing hormone (LH) thiab follicle-stimulating hormone (FSH) los ntawm kev thaiv cov pituitary GnRH receptors, yog li txo cov theem ntawm testosterone hauv lub cev. Nws tau dhau los ua cov cuab yeej tseem ceeb rau kev tsim tsiaj cov qauv ntawm androgen{2}}cov kab mob ntsig txog thiab tau siv dav hauv kev tshawb fawb kho mob, nrog rau cov ntawv thov tshwj xeeb raws li hauv qab no:
Tsim Cov Qauv Tsiaj ntawm Androgen-nyob ntawm Prostate Cancer
Nov yog thawj daim ntawv thov tshawb fawb scenario ntawm Degarelix. Cov kws tshawb fawb tuaj yeem ua rau subcutaneously inoculate prostate cancer cell kab (piv txwv li, LNCaP, VCaP) rau hauv cov qauv tsiaj xws li nas thiab nas, ua raws li intraperitoneal lossis subcutaneous txhaj ntawm Degarelix kom txo qis testosterone theem hauv cov tsiaj mus rau theem castration.
Cov qauv no tuaj yeem simulate cov tshuaj hormones- nyob ntawm lub xeev ntawm kev kho mob qog noj ntshav prostate, uas yog siv los tshawb txog cov teebmeem ntawm androgen deprivation ntawm cov qog loj hlob thiab metastasis, nrog rau cov txheej txheem hauv qab ntawm kev txhim kho cov qog cell tshuaj tiv thaiv. Piv nrog rau cov tsoos phais castration, Degarelix-induced chemical castration muaj qhov zoo ntawm kev ua haujlwm yooj yim, kev raug mob tsawg, thiab kev tswj hwm ntawm qib testosterone. Ntxiv mus, nws zam qhov tshwm sim ntawm testosterone flare cuam tshuam nrog GnRH agonists, uas ua rau muaj kev ruaj ntseg ntau dua.
Tsim kom muaj tsiaj qauv ntawm Txiv neej Climacteric Syndrome
Txiv neej climacteric syndrome yog ze ze rau qhov poob ntawm testosterone theem los ntawm kev laus. Sustained kev tswj hwm ntawm Degarelix mus rau nruab nrab- cov txiv neej laus nas lossis nas tuaj yeem txo lawv cov testosterone ntau ntau, yog li tsim kom muaj tus qauv pathological zoo ib yam li txiv neej climacteric syndrome.
Cov qauv no tuaj yeem siv los kawm txog cov txheej txheem pathological ntawm cov tsos mob tshwm sim los ntawm testosterone tsis muaj peev xwm, suav nrog kev ua menyuam yaus atrophy, txo cov pob txha pob txha pob txha, kev paub tsis meej, thiab kev hloov mus los. Lub caij no, nws muab qhov kev ntsuam xyuas kev ua tau zoo rau kev tshawb fawb thiab kev tsim cov tshuaj txhawm rau txhim kho txiv neej cov tsos mob, ua kom muaj kev sib piv ntawm kev kho mob ntawm cov neeg sib tw cov tshuaj thiab cov tshuaj testosterone hloov kho.
Tsim Cov Qauv Tsiaj ntawm Androgen-Cov Kab Mob Metabolic
Androgens ua lub luag haujlwm tseem ceeb hauv kev tswj hwm lub cev cov piam thaj thiab lipid metabolism nrog rau cov pob txha metabolism. Kev tsim cov androgen- cov qauv tsiaj tsis zoo sivDegarelixtso cai rau kev tshawb fawb txog kev sib raug zoo ntawm kev txo qis testosterone qib thiab cov kab mob metabolic xws li rog rog, insulin tsis kam, thiab osteoporosis.
Piv txwv li, hauv kev tshawb fawb osteoporosis, tus qauv no tuaj yeem ua rau pom qhov tshwm sim ntawm kev ua haujlwm ntawm osteoblast thiab hyperactive osteoclast muaj nuj nqi tshwm sim los ntawm androgen deficiency. Nws muab kev txhawb nqa kev sim rau kev txhim kho cov tshuaj tsom mus rau cov pob txha metabolism thiab tseem tuaj yeem siv los ntsuas qhov kev txhim kho ntawm kev tawm dag zog thiab kev noj zaub mov zoo ntawm androgen-deficiency osteoporosis.
Tsim Cov Qauv Tsiaj Ntawm Androgen-Cov Kab Mob Sib Kis
Androgens yog qhov tseem ceeb rau txoj kev loj hlob, kev loj hlob thiab kev ua haujlwm ntawm tus txiv neej lub cev xeeb tub. Kev txo qis ntawm testosterone ntau ntau tuaj yeem ua rau muaj ntau yam kab mob hauv lub cev tsis zoo, xws li spermatogenesis disorder, testicular atrophy, epididymal dysfunction thiab kev sib deev dysfunction. Degarelix, uas yog ib qho cuab yeej zoo los tswj cov qib testosterone, yog siv dav hauv kev tsim cov qauv tsiaj ntawm cov kab mob.
Hauv kev ua haujlwm tshwj xeeb, cov kws tshawb nrhiav tuaj yeem muab Degarelix ntawm cov tshuaj tsim nyog thiab chav kawm rau cov tub ntxhais hluas lossis cov neeg laus cov qauv tsiaj (xws li nas, nas thiab luav) kom txo qis lawv cov qib testosterone qib mus rau lub xeev pathological. Cov qauv no tuaj yeem raug simulate cov yam ntxwv ntawm cov kab mob ntawm cov txiv neej cov kab mob hauv cov kab mob tshwm sim los ntawm androgen deficiency, thiab yog siv los tshawb nrhiav cov txheej txheem tswj hwm ntawm androgens ntawm spermatogenesis, testicular thiab epididymal cell proliferation thiab sib txawv.
Tsis tas li ntawd, tus qauv no tseem muab qhov kev sim siab ntseeg siab rau kev tshawb fawb thiab kev txhim kho cov tshuaj kho mob rau androgen- cov kab mob hauv lub cev tsis zoo, xws li cov kab mob spermatogenesis- txhawb nqa tshuaj thiab kev npaj kho androgen hloov pauv, uas tuaj yeem soj ntsuam cov txiaj ntsig kho mob ntawm cov neeg sib tw tshuaj ntawm kev ua haujlwm ntawm kev ua me nyuam rov qab los.
Pharmacokinetic Properties
Absorption: A drug depot is formed for sustained release following subcutaneous injection, with high bioavailability. A steady state is rapidly achieved after administration of a 240 mg loading dose.Distribution: The volume of distribution is >1 L/kg for intravenous administration and >1000L rau kev txhaj tshuaj subcutaneous. Cov ntshav plasma protein khi tus nqi yog kwv yees li 90%, nrog rau kev faib tawm thoob plaws hauv lub cev cov kua dej thoob plaws hauv lub cev.Metabolism: Metabolized los ntawm peptide hydrolysis hauv cov kab mob hepatobiliary, tsis muaj cov plasma metabolites tseem ceeb. Nws tsis yog ib qho substrate/inhibitor/inducer ntawm CYP450 los yog P-glycoprotein, uas ua rau muaj kev pheej hmoo ntawm kev siv yeeb tshuaj -kev sib cuam tshuam tshuaj.Kev tshem tawm: Kev tshem tawm biphasic nrog lub davhlau ya nyob twg ib nrab- lub neej ntawm 43–53 hnub (kwv yees li ntawm 28 hnub ntawm kev saib xyuas li ntawm 8 hnub. mg). 20–30% ntawm cov tshuaj raug tshem tawm tsis hloov pauv hauv cov zis, thiab cov seem raug tshem tawm hauv cov quav raws li peptide fragments.
Toxicological yam ntxwv
Genotoxicity: Tsis muaj mutagenicity tau soj ntsuam hauv Ames kuaj, thiab tsis muaj cov teebmeem clastogenic tau kuaj pom hauv vitro thiab hauv vivo chromosomal assays.Reproductive toxicity: Tsiaj cov kev tshawb fawb tau pom tias muaj kev cuam tshuam ntawm fertility hauv cov txiv neej thiab poj niam nas. Txiv neej infertility tshwm sim los ntawm testosterone tsub kom yog thim rov qab. Contraindicated nyob rau hauv cov poj niam cev xeeb tub (FDA Pregnancy Category X).Carcinogenicity: Cov ntaub ntawv ntawm malignant lymphoma thiab squamous cell carcinoma tau tshaj tawm post-marketing; tsis muaj kev pheej hmoo mob qog noj ntshav tshwj xeeb tau pom nyob rau hauv tsis yog- kev tshawb fawb soj ntsuam.
Cia thiab Formulation yam ntxwv
Cov formulation yog lyophilized hmoov rau kev txhaj tshuaj, nrog rau cov xim tsis muaj xim thiab cov kuab tshuaj ntshiab. Lub lyophilized block muaj lub txee lub neej ntawm 2 xyoo ntawm 25℃.Cov tshuaj reconstituted ruaj khov rau 4 teev ntawm 25℃thiab yuav tsum tau siv tam sim; Nws tsis yog yuav tsum tau tov nrog lwm yam tshuaj.Tub kub- tswj kev thauj mus los, nrog rau kev zam ntawm kev ua nruj ua tsiv thiab khov-thaw mus los tiv thaiv kom tsis txhob muaj kev lom zem.
Tshuaj -Kev sib cuam tshuam tshuaj
Tsis muaj kev cuam tshuam rau CYP450 enzyme system, tsis muaj kev cuam tshuam metabolic nrog cov tshuaj feem ntau.Tej zaum ntev QTc ntu; Kev tshuaj xyuas electrocardiographic yuav tsum tau ua thaum koom nrog hauv chav kawm IA/III antiarrhythmics, methadone, thiab lwm yam tshuaj.Kev siv nrog electrolyte- hloov tshuaj yuav ua rau muaj kev pheej hmoo ntawm arrhythmias, yuav tsum tau saib xyuas cov qib poov tshuaj thiab magnesium.
Degarelixtau tsim los ntawm cov kws tshawb fawb los ntawm Shaanxi BLOOM Tech Co., Ltd. siv cov amino resin los ua cov cab cab pib thiab txuas txuas txuas cov Fmoc amino acids nyob rau hauv Digarec ib ntus los ntawm cov khoom sib xyaw ua ke -theem synthesis. Cov amino acid kawg siv yog Ac-D-2Nal{10}}OH. Tom qab cov tshuaj tiv thaiv condensation thiab deprotection cov tshuaj tiv thaiv, tau txais kev tiv thaiv tag nrho digarek peptide resin. Ntxiv acid cleavage thiab ether nag lossis daus tau ua kom tau cov crude digarec peptide. Tom qab chromatographic purification, acetic acid ntsev hloov, thiab khov-drying, cov khoom kawg yog digaric acetate. Cov kauj ruam ntxaws yog raws li nram no:
1. Kev npaj pib cov cab cab
(1) Nyob rau hauv cov xwm txheej nplawm, yaj cov amino resin hauv qhov tsim nyog ntawm cov kuab tshuaj, xws li dimethyl sulfoxide (DMSO). Xyuas kom meej tias cov amino resin yog yaj tag.
(2) Maj mam ntxiv cov tshuaj formaldehyde thiab tswj qhov kub ntawm ib ncig ntawm chav tsev kub. Nws tau pom tias cov amino resin maj mam ua kom khov.
(3) Txuas ntxiv stirring rau ib lub sij hawm ntawm lub sij hawm, ces ncuav lub amino resin mus rau hauv ib tug tsim nyog tus nqi ntawm methanol rau precipitate cov amino resin cab kuj.
(4) Lim thiab sau cov khib nyiab, ntxuav ob peb zaug nrog methanol, thiab tom qab ntawd ziab hauv qhov cub kom qhuav. Tau txais cov amino resin cab kuj.
2. Kev sib txuas ntawm cov amino acids
(1) Thauj cov amino resin cab kuj mus rau hauv lub reactor thiab ntxiv ib qho tsim nyog cov kuab tshuaj, xws li dimethylformamide (DMF), kom yaj tag cov amino resin.
(2) Maj mam ntxiv qhov tsim nyog ntawm Fmoc amino acids thiab coupling reagents, xws li Oxyma, nyob rau hauv stirring.
(3) Saib xyuas cov amino resin ua nkig, txuas ntxiv mus rau ib lub sijhawm, tom qab ntawd ncuav rau hauv cov kuab tshuaj uas tsim nyog, xws li methanol lossis ether, rau nag lossis daus.
(4) Lim thiab sau cov khib nyiab, ntxuav ob peb zaug nrog cov kuab tshuaj, thiab tom qab ntawd ziab hauv qhov cub kom qhuav. Tau txais cov amino resin ua ke nrog cov amino acids.
3. Lub condensation thiab deprotection ntawm peptide chains
(1) Thauj cov amino resin cab kuj ua ke nrog cov amino acids rau hauv lub reactor, ntxiv tus nqi tsim nyog ntawm cov kuab tshuaj thiab condensation tus neeg saib xyuas, xws li Diisopropylcarbodiimide (DIC) thiab 1-hydroxybenzotriazole (HOBt).
(2) Raws li kev sib xyaw ua ke, cov saw hlau peptide tau pom maj mam tsim thiab nplawm tsis tu ncua rau lub sijhawm.
(3) Ntxiv qhov tsim nyog ntawm cov tshuaj tiv thaiv kev tiv thaiv, xws li trifluoroacetic acid (TFA), rau cov tshuaj tiv thaiv kom tshem tawm cov pab pawg tiv thaiv los ntawm cov saw peptide.
(4) Tom qab ib lub sij hawm ntawm cov tshuaj tiv thaiv, txiav cov peptide saw tawm ntawm cov amino resin. Ntxuav nrog cov kuab tshuaj xws li ether lossis acetone, thiab tom qab ntawd ziab hauv qhov cub kom qhuav. Kev tiv thaiv tag nrho digarek peptide resin.
4. Acid hydrolysis txiav thiab ether nag lossis daus
(1) Sau tag nrho cov kev tiv thaiv digarec peptide resin rau hauv lub reactor thiab ntxiv cov kua qaub hydrolysis reagent, xws li hydrochloric acid.
(2) Nyob rau hauv cov xwm txheej nplawm, tom qab ib lub sij hawm ntawm cov tshuaj tiv thaiv, nws tau pom tias peptide chains raug txiav tawm ntawm cov amino resin.
(3) Ntxiv qhov tsim nyog ntawm ether rau cov tshuaj tiv thaiv kom cia cov saw peptide nyob hauv ether.
(4) Lim thiab sau cov khib nyiab, ntxuav ob peb zaug nrog ether, thiab tom qab ntawd ziab hauv qhov cub kom qhuav. Tau txais crude digaric peptide.
5. Chromatographic purification, acetic acid ntsev hloov, thiab khov - ziab
Module npe
(1) Dissolve cov crude digaric peptide nyob rau hauv ib tug tsim nyog tus nqi ntawm cov kuab tshuaj, xws li ib tug sib tov ntawm methanol thiab dej (qhov piv yuav raug kho raws li qhov tseeb). Tom qab ntawd, cov tshuaj yog sib cais los ntawm chromatography siv silica gel kem los yog rov qab theem C18 kem. Cov theem ntawm lub xov tooj ntawm tes yog kev sib xyaw ntawm methanol thiab dej (qhov sib piv yog kho raws li qhov xwm txheej tiag), thiab cov eluent tau sau thaum nws ntws tawm. Cov kua sau tau yog concentrated thiab tom qab ntawd raug rau acetic acid ntsev hloov ua haujlwm. Txoj kev tshwj xeeb yog ntxiv cov kua sau rau hauv acetic acid tov, do rau ib lub sijhawm, lim thiab cais cov khoom, ntxuav nws nrog cov kuab tshuaj organic ob peb zaug, thiab tom qab ntawd ziab nws hauv lub tshuab nqus tsev kom tau cov khoom acetic acid digaric.
(2) Ntxiv purify cov khoom ntawm digaric acetate los ntawm chromatographic purification technology. Kev ua kom huv huv tuaj yeem ua tau siv cov kev sib cais chromatographic xws li silica gel kem thiab thim rov qab theem C18 kem. Los ntawm kev kho qhov sib piv ntawm cov theem ntawm lub xov tooj ntawm tes thiab qhov ntim ntawm eluent, cov khoom ntawm digaric acetate tuaj yeem sib cais ntxiv thiab huv si.
(3) Ua acetic acid ntsev hloov pauv ntawm cov khoom purified digaric acetate los txhim kho nws cov solubility thiab stability. Txoj kev tshwj xeeb yog kom yaj cov khoom ntawm digaric acetate nyob rau hauv qhov tsim nyog tus nqi ntawm acetic acid tov, do rau ib lub sij hawm ntawm lub sij hawm, lim thiab cais cov khoom, ntxuav nrog organic solvent ob peb zaug, thiab ces qhuav nyob rau hauv lub tshuab nqus tsev ziab qhov cub. Tau txais qhov kawg acetic acid digaric khoom.
(4) Thaum kawg, ua kom khov- ziab ntawm cov khoom acetic acid digaric. Kev ziab kom qhuav tuaj yeem tshem tawm cov dej ntau dhau thiab cov kuab tshuaj, txhim kho cov purity thiab stability ntawm cov khoom. Txoj kev tshwj xeeb yog muab cov khoom siv acetic acid digaric tso rau hauv khov - tshuab ziab khaub ncaws thiab ziab nws nyob rau hauv qhov kub thiab txias. Cov tshuaj acetic acid digaricDegarelixua tiav los ntawm khov- ziab tuaj yeem khaws cia thiab siv tau ntev.
FAQ
Cov tshuaj degarelix siv rau dab tsi?
Degarelix yog tshuaj hormonal kho. Nws tseem hu ua Firmagon. Nws yog sivkho mob qog noj ntshav prostate. Tej zaum nws yuav siv tau los kho lwm yam qog noj ntshav.
Puas yog degarelix tib yam li Lupron?
Degarelix (Firmagon) zoo li leuprolide (Lupron Depot) hauv kev txo qis thiab txhawb nqa qib castrate ntawm testosterone., tab sis thaum thawj xyoo ntawm kev kho mob, cov neeg mob tau txais degarelix muaj qhov pheej hmoo ntawm PSA kev loj hlob lossis tuag ntau dua li cov neeg tau txais leuprolide, raws li kev tshawb fawb qhia ...
Dab tsi yog cov kev mob tshwm sim ntawm degarelix?
Feem ntau cov kev phiv tshwm sim tau tshaj tawm hauv Ntau dua lossis sib npaug li 10% ntawm cov neeg mob yog qhov chaw txhaj tshuaj (piv txwv li, mob, erythema, o, induration, lossis o), pyrexia, kub dej, poob phaus lossis nce, qaug zog, thiab nce qib hauv cov ntshav siab ntawm hepatic transaminases thiab gamma{1}Glutamyltransferase (Glutamyltransferase).
Puas yog degarelix tib yam li Zoladex?
Zoladex (goserelin) thiab Firmagon (degarelix) yog ob qho tib si siv los kho mob qog noj ntshav prostate, tab sis lawv ua haujlwm sib txawv.. Zoladex yog ib qho gonadotropin- tso tawm cov tshuaj hormones (GnRH) agonist, uas txhais tau hais tias nws ua raws li cov tshuaj hormones los txo qis testosterone thiab estrogen.
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