Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm abarelix acetate hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo abarelix acetate muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Abarelix acetate hmoov, tseem hu ua abarelix hauv Suav, muaj cov qauv molecular C72H95ClN14O14 thiab CAS 183552-38-7. Nws yog ib qho hluavtaws peptide compound uas belongs rau chav kawm ntawm gonadotropin-tso hormone (GnRH) antagonists thiab cov tshuaj tiv thaiv kab mob. Nws yog siv nyob rau hauv kev kho mob raws li ib tug tshuaj tiv thaiv qog, tshwj xeeb yog cais raws li LHRH inhibitors, nrog ATC code L02BX01.
Abarelix Acetate COA
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| Certificate of Analysis | ||
| Compound npe | Abarelix acetate hmoov | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 183552-38-7 | |
| Ntau | 53g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090056 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| 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% | 0.31% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.62% |
| 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% | 99.80% |
| Ib leeg impurity | <0.8% | 0.44% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 209 |
| 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 | 5 12 ppm |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab 2-8 degree | |
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| Chemical Formula: | C72H95ClN14O14 |
| Exact Mass: | 1415 |
| Molecular Luj: | 1416 |
| m/z: | 1415 (100.0%), 1416 (77.9%), 1417 (32.0%), 1417 (29.9%), 1418 (24.9%), 1419 (9.6%), 1418 (7.5%), 1416 (4.8%), 1417 (4.0%), 1417 (2.9%), 1418 (2.2%), 1420 (2.2%), 1418 (1.7%), 1418 (1.4%), 1419 (1.2%), 1419 (1.1%), 1416 (1.1%) |
| Elemental Analysis: | C, 61,07; H, 6,76; Cl, 2,50; N, 13,85; 15.82 Nws |
Abarelix acetate hmoovyog ib qho hluavtaws peptide uas muaj zog tiv thaiv kev ua haujlwm, koom nrog hauv chav kawm ntawm gonadotropin- tso cov tshuaj hormone (GnRH) antagonists, uas ua lub luag haujlwm tseem ceeb hauv kev kho mob qog noj ntshav prostate.
Cov yam ntxwv tseem ceeb ntawm Abarik
Abarik yog ib qho kev sib xyaw ua ke peptide nrog cov qauv molecular C ₇₂ H ₉₅ ClN ₁₄ O ₁₄, thiab qhov hnyav molecular ntawm 1416.08. Nws zoo nkaus li dawb rau cov hmoov dawb uas muaj purity ntawm 95% mus rau 99%, thiab tuaj yeem txheeb xyuas los ntawm HPLC-DAD txoj kev. Abarek muaj cov ntshav plasma protein ntau khi tus nqi (96% ~ 99%) thiab dav dav hauv lub cev, nrog lub davhlau ya nyob twg pom meej qhov ntim ntawm 4040 ± 1607L. Nws cov metabolism feem ntau yog ua los ntawm peptide bond hydrolysis, thiab tsis muaj pov thawj los qhia tias cytochrome P450 koom nrog hauv nws cov txheej txheem metabolic.
Tom qab txhaj tshuaj intramuscular hauv tib neeg lub cev, kwv yees li 13% ntawm cov qauv tshuaj raug tso tawm nrog cov zis, thiab tsis muaj lwm yam metabolites raug kuaj pom hauv cov zis. Lub raum tshem tawm ntawm 100mg txhaj yog 14.4L / d (los yog 10mL / min). Cov yam ntxwv no muab lub hauv paus rau cov teebmeem pharmacological thiab metabolic tshem tawm ntawm Abarik hauv lub cev.
Source: Chemicalbook (Booker Chemical Network), Pharmaceutical Online.
Inhibition ntawm LH thiab FSH secretion
Vim nws txoj kev khi rau GnRH lees txais, uas thaiv cov teeb liab hloov ntawm GnRH, qhov tso tawm ntawm LH thiab FSH los ntawm lub caj pas anterior pituitary yog inhibited. Qhov txo qis ntawm LH thiab FSH ncaj qha cuam tshuam rau kev ua haujlwm ntawm gonads. Hauv cov txiv neej, cov noob qes yog cov gonads tseem ceeb, thiab LH yog cov tshuaj hormones tseem ceeb uas ua rau cov qog nqaij hlav hauv nruab nrog cev kom zais cov testosterone.
Thaum LH secretion txo qis, lub peev xwm ntawm testicular interstitial hlwb los synthesize thiab secrete testosterone txo, ua rau txo qis hauv plasma testosterone concentration. Ib yam li ntawd, FSH kuj tseem muaj feem cuam tshuam rau kev ua haujlwm spermatogenic ntawm cov qog ntshav. Txo FSH secretion tuaj yeem cuam tshuam cov phev ntau lawm, tab sis hauv kev kho mob qog noj ntshav prostate, lub hom phiaj tseem ceeb yog txo qis qib testosterone.
Source: ChemicalBook (Booker Chemical Network), Tuam Tshoj Pharmaceutical Information Query Platform
Kev kho mob ntawm kev txo qis testosterone qib ntawm prostate cancer
Prostate cancer yog ib qho androgen nyob ntawm qog, thiab testosterone thiab lwm yam androgens ua lub luag haujlwm tseem ceeb hauv kev tshwm sim, kev loj hlob, thiab kev loj hlob ntawm prostate cancer. Testosterone tuaj yeem qhib ntau txoj hauv kev los ntawm kev khi rau cov neeg txais androgen hauv cov qog nqaij hlav qog nqaij hlav prostate, txhawb kev mob qog noj ntshav, muaj sia nyob, thiab metastasis. Yog li ntawd, txo qis testosterone qib hauv lub cev yog ib qho ntawm cov tswv yim tseem ceeb rau kev kho mob qog noj ntshav prostate.
Abarek ua tau zoo txo qhov muaj peev xwm ntawm cov noob qes kom zais cov testosterone los ntawm inhibiting qhov tso tawm ntawm LH thiab FSH, ua rau txo qis hauv plasma testosterone concentration. Cov nyhuv no ntawm kev txo qis testosterone yog hu ua castration, zoo ib yam li kev phais tshem tawm ntawm cov noob qes (kev phais castration) lossis kev siv tshuaj los tiv thaiv cov qog nqaij hlav (tshuaj castration). Piv nrog rau cov tshuaj GnRH agonists, nws muaj qhov tshwj xeeb zoo.
Ib txwm siv GnRH agonists tuaj yeem ua rau luv luv ntawm LH thiab FSH qib thaum pib siv, ua rau muaj kev nce ntxiv tom qab los ntawm kev txo qis hauv qib testosterone, txheej txheem hu ua rebound. Thaum lub sij hawm theem ntawm qib siab testosterone, nws yuav ua rau muaj kev loj hlob thiab kev sib kis ntawm cov qog nqaij hlav qog nqaij hlav prostate, ua rau lub cev tsis zoo. Raws li ib tug GnRH antagonist, nws ncaj qha inhibits LH secretion yam tsis ua rau ib tug rebound nyob rau hauv testosterone qib, thiab yuav txo tau sai npaum li cas testosterone, yog li ntawd zoo dua tswj cov kev loj hlob ntawm prostate cancer.
Source: Chemicalbook, Xiaohe Health, Pharmaceutical Online
Txo cov tsos mob: Hauv cov neeg mob uas muaj mob qog noj ntshav siab, cov tsos mob hnyav feem ntau tshwm sim vim cov qog nqaij hlav metastasis thiab ntxeem tau, xws li mob pob txha hnyav los ntawm cov qog pob txha metastasis, ureteral lossis zais zis qhov hluav taws xob cuam tshuam los ntawm kev cuam tshuam hauv zos lossis cov kab mob metastatic, thiab muaj peev xwm ua rau puas hlwb los ntawm cov qog metastasis. Los ntawm kev txo qis testosterone qib thiab inhibiting kev loj hlob thiab kev sib kis ntawm cov qog nqaij hlav cancer prostate, cov tsos mob no tuaj yeem txo qis.
Piv txwv li, hauv kev tshawb fawb soj ntsuam ntawm cov neeg mob uas muaj cov tsos mob ntawm tus mob prostate siab heev, 15 cov neeg mob uas muaj pob txha metastases tau ntsib kev mob nyem tom qab 12 lub lis piam ntawm kev kho mob, thiab qhov ua tau zoo, ntau npaum li cas, thiab zaus ntawm kev siv tshuaj loog txo qis; Kaum peb tus neeg mob uas muaj lub zais zis thaiv qhov tso zis thiab tso zis tso zis, 10 tus neeg tau tshem cov hlab ntsha tom qab 12 lub lis piam; Ntawm 8 tus neeg mob uas muaj tus txha caj qaum lossis epidural metastases tab sis tsis muaj cov tsos mob ntawm lub paj hlwb, tsis muaj leej twg pom cov tsos mob puas hlwb.
Kev kho mob Palliative: feem ntau yog siv rau kev kho mob palliative ntawm cov tsos mob ntawm prostate cancer (PCA) uas tsis haum rau kev txais luteinizing hormone tso tawm hormone (LHRH) agonist therapy thiab tsis kam phais phais, thiab muaj ib lossis ntau dua ntawm cov xwm txheej saum toj no. Lub hom phiaj ntawm kev saib xyuas palliative yog txhawm rau txo qhov mob ntawm cov neeg mob, txhim kho lawv lub neej zoo, thiab ua kom muaj sia nyob ntev los ntawm kev tswj hwm kev mob qog noj ntshav prostate, muab kev kho mob tseem ceeb rau cov neeg mob no.
Zam kev pheej hmoo ntawm kev phais: Rau qee cov neeg mob uas tsis haum rau kev phais lossis tsis kam phais,Abarelix acetate hmoovmuab ib txoj kev uas tsis yog - phais ntawm castration. Piv nrog rau kev phais castration, tshuaj castration muaj qhov zoo ntawm qhov tsis muaj kev cuam tshuam thiab thim rov qab, uas tuaj yeem txo qhov mob thiab kev pheej hmoo ntawm cov teeb meem tshwm sim los ntawm kev phais thiab txhim kho lub neej zoo ntawm cov neeg mob.
Source: ChemicalBook, Tuam Tshoj Pharmaceutical Information Query Platform, Xiaohe Health.
Chemical Structure
Abarek yog ib qho decapeptide nrog cov amino acid ib ntus uas muaj ib tsab ntawv ib ntus: Ac - DNal - DpClPhe - D3Pal - Ser - Asn - Tyr - DLys - Leu {- 1} Pro - NH ₂; Peb tsab ntawv ib ntus: Ac - D - Nal - D - pCl - Phe - D - 3Pal - Ser - Asn - Tyr - D {{22} {24} Ly - Pro - D - Ala - NH ₂.
Los ntawm txoj kev xav ntawm cov yam ntxwv ntawm cov yam ntxwv:
Nws N-terminus yog acetylated (Ac -), uas ua rau kom muaj kev ruaj ntseg ntawm polypeptide thiab tiv thaiv degradation los ntawm enzymes xws li aminopeptidases. Cov qauv muaj ntau yam D-configured amino acids, xws li D-Nal (D-naphthylalanine), D-pClPhe (D-p-chlorophenylalanine), D-3Pal (D-3{Lpyridine), (D-}lysine), thiab D-Ala (D{18}}alanine). Piv nrog rau L-configuration amino acids, D-configuration amino acids hloov lub spatial conformation ntawm peptides, ua rau lawv tshwj xeeb khi rau gonadotropin-tso cov tshuaj hormones (GnRH) txais nrog muaj zog binding affinity thiab tsawg dua yuav raug hloov los ntawm endogenous GnRH kev sib tw.
Lub caij no, phenolic hydroxyl pawg ntawm Tyr (tyrosine) residues tuaj yeem koom nrog hauv kev tsim cov hydrogen bonds ntawm molecules, cuam tshuam rau lawv cov folding thiab kev ua si. Lub xub ntiag ntawm Pro (proline) residues nyob rau hauv peptide chains ua rau kev khoov tshwj xeeb, uas yog ib qho tseem ceeb rau kev tswj tag nrho spatial conformation ntawm cov khoom thiab nws affinity thiab tshwj xeeb rau kev khi rau cov neeg txais.
R & D thiab kev ua lag luam
Abarelix acetate hmoovtau tsim los ntawm Praecis Pharmaceuticals hauv Tebchaws Meskas. Thaum Lub Ib Hlis 30, 2004, nws tau sau thawj zaug hauv Tebchaws Meskas. Nyob rau hauv tib lub xyoo, nws txoj cai los kho mob qog noj ntshav hauv Australia, Europe, Middle East, New Zealand, Russia, thiab South Africa raug xa mus rau Shilling Company. Txawm li cas los xij, vim nws qhov siab ntawm cov tshuaj tiv thaiv hypersensitivity tshwm sim los ntawm kev tso tawm histamine, nws tau raug tshem tawm los ntawm Asmeskas kev lag luam los ntawm FDA hauv 2005.
Cim npe nrov: Abarelix acetate, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom