Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm ligandrol (lgd-4033 capsule) hauv Suav teb. Txais tos rau cov lag luam wholesale zoo zoo ligandrol (lgd-4033 capsule) muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Ligandrol (LGD-4033 Capsule)yog lub qhov ncauj xaiv androgen receptor modulator (SARM), encapsulated nyob rau hauv capsules rau meej npaum li cas thiab kev tswj hwm. Muab piv rau cov ntaub ntawv ua kua lossis hmoov, cov tshuaj ntsiav muaj kev ruaj ntseg zoo dua, kev txav mus los, thiab kev zam ntawm kev pheej hmoo ntawm cov kuab tshuaj lom. LGD-4033 xaiv activates androgen receptors hauv cov leeg thiab pob txha, txhawb cov txheej txheem anabolic, ua kom lub cev tsis muaj zog thiab lub zog, thaum txo cov kev mob tshwm sim hauv cov ntaub so ntswg xws li prostate thiab siab. Cov kev tshawb fawb Preclinical tau pom tias LGD-4033 capsules tuaj yeem txhim kho cov leeg nqaij thiab pob txha ntawm 5 hnub. Lub neej ib nrab yog kwv yees li 24-36 teev thiab nws tsim nyog rau kev tswj hwm txhua hnub.Vim tsis muaj cov ntaub ntawv kev nyab xeeb mus ntev, nws tsis tau pom zoo los ntawm FDA thiab tsuas yog muag rau kev tshawb fawb.
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Ligandrol (LGD-4033) COA
Core Potential nyob rau hauv Kev Kho Mob ntawm Muscular Atrophy
Cov leeg nqaij atrophy yog hais txog cov tsos mob uas tshwm sim los ntawm qhov txo qis ntawm cov leeg nqaij thiab cov leeg nqaij tsis muaj zog los ntawm ntau yam xws li kev laus, kab mob, thiab kev raug mob, uas cuam tshuam rau cov neeg mob lub cev muaj zog thiab lub neej zoo.Ligandrol (LGD-4033 Capsule)yog thawj zaug tsim los daws qhov kev xav tau kho mob no. Nws cov txheej txheem tseem ceeb ntawm kev ua yog nyob rau hauv tshwj xeeb activating androgen receptors nyob rau hauv cov leeg nqaij los txhawb cov protein synthesis thiab inhibit cov leeg catabolism, thaum alleviating oxidative stress-induced puas hlwb hlwb thiab txhim kho cov leeg cell viability.
Hauv kev tshawb fawb preclinical, nws tau pom tias muaj txiaj ntsig zoo rau cov leeg nqaij atrophy los ntawm ntau yam etiologies. Rau hnub nyoog -txog sarcopenia, tib neeg androgen theem poob qis nrog lub hnub nyoog, ua rau cov leeg nqaij tsis zoo, thiab nws tuaj yeem thim rov qab cov txheej txheem no los ntawm kev ua raws li cov teebmeem anabolic ntawm androgens. Rau cov leeg nqaij dystrophy, nws tuaj yeem ncua qhov kev loj hlob ntawm cov leeg nqaij fibrosis thiab txhim kho cov neeg mob lub cev muaj zog los ntawm kev txhim kho cov tshuaj tiv thaiv -apoptotic muaj peev xwm ntawm cov leeg nqaij.
Ntawm cov neeg mob qog noj ntshav, kev kho hluav taws xob thiab tshuaj khomob feem ntau ua rau cov leeg mob hnyav heev; Cov kev sim hauv vitro tau pom tias nws tuaj yeem txo qhov myotoxicity thiab apoptosis vim los ntawm cov tshuaj siv tshuaj xws li cisplatin, muab kev txhawb nqa rau cov neeg mob qog noj ntshav kom tswj tau cov leeg nqaij.
Kev tiv thaiv thiab kho tus nqi rau Osteoporosis
Osteoporosis yog tus cwj pwm los ntawm kev txo cov pob txha loj thiab cov pob txha tsis zoo, uas yooj yim ua rau muaj kev pheej hmoo ntawm pob txha, thiab tshwj xeeb tshaj yog muaj nyob rau hauv nruab nrab - cov neeg laus thiab cov neeg laus thiab cov neeg mob uas muaj kab mob ntev. Los ntawm kev tswj cov pob txha metabolic txoj hauv kev, nws nthuav tawm cov pob txha tseem ceeb - tiv thaiv cov teebmeem, muab cov kev taw qhia tshiab rau kev tiv thaiv thiab kho pob txha.
Nws cov txheej txheem ntawm kev ua haujlwm feem ntau yog tshwm sim hauv ob yam: txhawb cov pob txha tsim thiab inhibiting pob txha resorption. Raws li tus androgen receptor agonist, cov khoom lag luam tuaj yeem ua rau cov pob txha pob txha, txhim khu kev ua haujlwm osteoblast, txhawb kev tsim cov pob txha periosteal, thiab txhim kho microstructure ntawm cov pob txha, yog li ua kom cov pob txha pob txha ntom ntom (BMD). Tib lub sijhawm, nws tuaj yeem cuam tshuam cov pob txha resorption muaj nuj nqi ntawm osteoclasts, txo cov pob txha poob, thiab tswj cov pob txha homeostasis. Qhov kev tswj hwm ob txoj cai no txawv nws ntawm cov tshuaj tiv thaiv kab mob -osteoporotic, vim nws tuaj yeem ua rau cov pob txha tsim thiab khaws cov pob txha uas twb muaj lawm.
Cov kev tshawb fawb ua ntej tau pom tias LGD-4033 tuaj yeem txhim kho cov pob txha mechanical zog ntawm cov tsiaj sim thiab txo qhov tshwm sim ntawm pob txha. Rau cov kab mob osteoporosis thib ob tshwm sim los ntawm kev hloov pauv hormonal, kab mob ntev lossis kev siv tshuaj kho mob, xws li cov pob txha puas tsuaj los ntawm kev siv cov glucocorticoid ntev, Ligandrol kuj tuaj yeem tiv thaiv kev tiv thaiv los ntawm kev tswj cov pob txha metabolic.
Daim Ntawv Thov Kev Pom Zoo hauv Kev Tiv Thaiv Cachexia
Cachexia yog ib qho teeb meem metabolic tsis meej uas tshwm sim hauv cov neeg mob uas muaj kab mob hnyav xws li mob qog noj ntshav, AIDS, kab mob raum ntev, thiab kab mob pulmonary mob ntev. Nws yog tus cwj pwm los ntawm kev poob phaus, cov leeg nqaij atrophy, thiab rog rog, uas cuam tshuam rau cov neeg mob kev kho mob siab ntev thiab lub sijhawm muaj sia nyob. Tam sim no, tsis muaj txoj hauv kev kho mob zoo, thiab nws tau dhau los ua cov tshuaj muaj peev xwm rau kev tiv thaiv thiab kev cuam tshuam ntawm cachexia los ntawm kev tsim txiaj ntawm nws cov leeg nqaij muaj zog.
Cov txheej txheem tseem ceeb ntawm cov txheej txheem ntawm cachexia yog metabolic tsis txaus los ntawm kev tso tawm ntau dhau ntawm cov kab mob inflammatory, ua rau hyperactive protein catabolism thiab inhibited anabolism. Los ntawm activating androgen receptors nyob rau hauv cov nqaij cov nqaij, nws ho txhim khu cov protein synthesis efficiency, tiv thaiv inflammatory yam tshwm sim - nruab nrab ntawm cov nqaij ntshiv, thiab nyob rau tib lub sij hawm nce cov neeg mob lub qab los noj mov thiab lub zog kom tau txais kev noj haus zoo. Rau cov neeg mob qog noj ntshav, nws tuaj yeem tsis tsuas yog txo cov leeg nqaij nkim los ntawm kev siv hluav taws xob thiab tshuaj khomob, tab sis kuj tseem txhim kho lub cev muaj zog thiab ua raws li kev kho mob; Hauv cov neeg mob AIDS, nws tuaj yeem txo cov leeg nqaij atrophy thiab kev tiv thaiv kev ua haujlwm poob qis vim yog kis kab mob, thiab txhim kho lub neej zoo.
Muaj peev xwm tiv thaiv - mob ntshav qab zib cov teebmeem thiab cov txheej txheem
Ntxiv nrog rau nws cov kev tiv thaiv cov leeg nqaij thiab pob txha, cov kev tshawb fawb hauv xyoo tas los no tau pom tias cov khoom lag luam kuj muaj qee yam kev tiv thaiv - mob ntshav qab zib, tshwj xeeb tshaj yog qhia tias muaj txiaj ntsig zoo hauv kev txhim kho cov tsos mob ntawm hom 2 mob ntshav qab zib. Nws cov txheej txheem ntawm kev ua haujlwm feem ntau yog tsom mus rau pancreatic islet muaj nuj nqi tiv thaiv thiab kev tswj hwm cov tshuaj insulin.
Cov kab mob pancreatic tsis zoo -cov haujlwm ntawm tes yog ib qho tseem ceeb hauv kev tshwm sim thiab kev loj hlob ntawm hom 2 mob ntshav qab zib. Nws tuaj yeem tiv thaiv kab mob pancreatic - ntawm tes ua haujlwm los ntawm kev tiv thaiv kev puas tsuaj ntawm cov kab mob pancreatic. Kev sim hauv vitro tau lees paub tias nws tuaj yeem cuam tshuam streptozotocin -induced pancreatic islet cell puas, txo cov cell apoptosis, thiab tib lub sijhawm txhawb kev tso tawm insulin los txhim kho islet secretory function. Ntxiv rau,Ligandrol (LGD-4033 Capsule)tuaj yeem txhim kho lub cev cov tshuaj insulin rhiab heev, txhawb nqa thiab siv cov piam thaj los ntawm cov ntaub so ntswg (xws li cov leeg thiab cov rog), txo cov ntshav qabzib sai, thiab txo qis cov tshuaj insulin.
Chemical Nature thiab Molecular Design
LGD-4033 yog ib qho tsis yog-steroidal selective androgen receptor modulator (SARM), nrog cov mis mos molecular C₁₄H₁₂F₆N₂O thiab molecular hnyav 338.25 g/mol. Nws cov qauv tseem ceeb muaj ib lub nplhaib pyrrolidine thiab ob pawg trifluoromethyl, uas muab nws siab lipid solubility thiab stability. Tsis zoo li cov tshuaj anabolic steroids (xws li testosterone), LGD-4033 xaiv activates androgen receptors nyob rau hauv cov leeg thiab cov pob txha, zam dhau stimulation ntawm cov ntaub so ntswg uas tsis yog hom phiaj xws li prostate thiab siab, yog li txo cov kev mob tshwm sim (xws li prostate hypertrophy, plaub hau poob, thiab lwm yam).
Cov txheej txheem tsim khoom thiab cov kauj ruam tseem ceeb
Lub synthesis ntawm LGD-4033 pib nrog cov khoom siv tshuaj lom neeg yooj yim, xws li cesium fluoride, trimethylsilane, potassium hydroxide, thiab lwm yam. Cov khoom siv raw no tau siv tshuaj lom neeg los tsim cov khoom nruab nrab, uas yog tom qab ntawd txuas ntxiv mus rau hauv lub hom phiaj molecule. Lub purity ntawm qhov tseem ceeb intermediates ncaj qha cuam tshuam qhov zoo ntawm cov khoom kawg, yog li nruj kev ntsuam xyuas siv high-performance kua chromatography (HPLC) los yog roj chromatography (GC) yog tsim nyog.
Lub synthesis ntawm LGD-4033 muaj ntau yam kev cuam tshuam cov organic, nrog rau fluorination, cyclization, nitration, thiab lwm yam. Txhua kauj ruam cov tshuaj tiv thaiv yuav tsum tau tshwj xeeb kub, siab, thiab catalyst tej yam kev mob los xyuas kom meej yield thiab purity. Piv txwv li, kev qhia txog cov pab pawg trifluoromethyl yuav tsum tau ua ntawm qhov kub thiab txias uas siv cov tshuaj fluorinating reagents kom tsis txhob muaj qhov tshwm sim ntawm kev phiv.
Cov khoom nyoos LGD-4033 yuav tsum tau ntxuav los ntawm recrystallization lossis kem chromatography kom tshem tawm impurities. Kev xaiv cov kuab tshuaj crystallization (xws li ethanol, acetone) yuav tsum coj mus rau hauv tus account solubility thiab crystallization efficiency. Cov khoom purified yuav tsum ncav cuag ib tug purity ntawm ntau dua los yog sib npaug rau 98% kom tau raws li qhov yuav tsum tau ntawm kev tshawb fawb los yog kev kho mob daim ntawv thov.
Cov khoom xyaw xaiv: LGD-4033 yog cov hmoov hydrophobic, thiab nws yuav tsum tau tov nrog excipients (xws li microcrystalline cellulose, lactose) los txhim kho flowability. Capsule shells feem ntau yog ua los ntawm gelatin lossis hydroxypropyl methylcellulose (HPMC) kom tsis txhob muaj kev cuam tshuam tshuaj.
Cov txheej txheem sau: Siv lub tshuab tsis siv neeg lub tshuab ua kua filling tshuab los tswj cov ntsiab lus yuam kev ntawm txhua lub tshuaj ntsiav hauv ± 5%. Qhov chaw ntim khoom yuav tsum muaj cov av noo tsawg (RH <30%) kom tiv thaiv cov hmoov los ntawm absorbing noo noo thiab caking.
Ntim thiab Cia: Cov tshuaj ntsiav ua tiav yuav tsum tau muab ntim rau hauv cov ntawv ci txhuas los yog siab - ntom polyethylene (HDPE) fwj, khaws cia rau hauv lub teeb- tiv thaiv ib puag ncig ntawm -20 degree, thiab khaws cia rau lub sijhawm siv tau ntawm 2-3 xyoos.
Kev Tswj Xyuas Zoo thiab Cov Qauv
Kev kuaj purity
Lub purity ntawmLigandrol (LGD-4033 Capsule)tau txiav txim los ntawm HPLC. Lub ntsiab ncov cheeb tsam suav nrog ntau dua lossis sib npaug li 98%, ib qho impurity Tsawg dua lossis sib npaug li 0.5%, thiab tag nrho impurity Tsawg dua lossis sib npaug li 1.0%.
Residual solvent tsom xam
Cov seem ntawm cov kuab tshuaj organic (xws li methanol thiab dichloromethane) siv nyob rau hauv cov txheej txheem synthesis yuav tsum ua tau raws li tus qauv thoob ntiaj teb rau cov tshuaj excipients (ICH cov lus qhia), xws li methanol residue tsawg dua lossis sib npaug li 3000 ppm.
Microbial txwv
Rau kev npaj tsis muaj menyuam, tag nrho cov kab mob yuav tsum tau tswj tsawg dua lossis sib npaug li 1000 cfu / g, pwm thiab cov poov xab tsawg dua lossis sib npaug li 100 cfu / g kom ntseeg tau tias cov khoom muaj kev nyab xeeb.
Kev kuaj kev ruaj ntseg
Accelerated stability test (40℃/ 75% RH) thiab ntev - lub sij hawm stability test (25℃/ 60% RH) yuav tsum ua pov thawj tias qhov zoo ntawm cov khoom yog ruaj khov nyob rau hauv lub validity lub sij hawm, thiab cov khoom degradation yuav tsum tsis txhob ntau tshaj 5% ntawm tus nqi cim.
Raws li txoj cai
LGD-4033 tau teev npe raws li cov khoom txwv tsis pub los ntawm Ntiaj Teb Kev Tiv Thaiv -Doping Agency (WADA), thiab cov neeg ncaws pob uas siv nws yuav raug nplua. Nws cov kev tshawb fawb soj ntsuam tsuas yog siv rau kev kho mob xws li cov leeg nqaij atrophy thiab osteoporosis, thiab nws txoj kev siv tshuaj tsis raug cai.
Daim ntawv tso cai tsim khoom
Kev tsim khoom LGD-4033 yuav tsum tau txais GMP daim ntawv pov thawj rau kev tsim tshuaj thiab kev pom zoo los ntawm cov cai tswj hwm tshuaj (xws li FDA, EMA). Kev tsim khoom thiab kev muag khoom tsis pom zoo yuav cuam tshuam txog kev ua txhaum cai.
Kev Tiv Thaiv Kev Txawj Ntse
Lub patent rau LGD-4033 yog tuav los ntawm Viking Therapeutics. Lwm lub tuam txhab yuav tsum tau txais kev tso cai los tsim nws raws cai. Patent infringement foob yog ib qho kev pheej hmoo hauv kev lag luam, thiab kev pheej hmoo tuaj yeem raug txo los ntawm patent zam tsim los yog kev sib koom tes tsim kho.
Kev ua lag luam xwm txheej thiab yav tom ntej Trends
Kev Ua Lag Luam
LGD-4033 muaj qhov xav tau zoo hauv cov chaw qoj ib ce thiab kev ua kis las, tab sis muaj teeb meem ntawm qhov tsis sib xws hauv cov kev muag khoom tsis raug cai. Kev tshawb fawb-qib cov khoom (nrog rau purity ntau dua lossis sib npaug li 98%) yog kim dua (kwv yees li 500-1000 yuan / g), thaum cov khoom lag luam qib (nrog purity ntawm 90-95%) yog pheej yig dua (kwv yees 200-500 yuan / g).
Technology Innovation
Nruam-tshuaj lom neeg siv tshuab tuaj yeem txhim kho kev sib xyaw ua haujlwm thiab txo cov kev siv hnyav; biocatalytic synthesis tuaj yeem dhau los ua kev taw qhia tshiab rau kev tsim ntsuab. Tsis tas li ntawd, cov qauv tshiab (xws li nanocrystals, liposomes) tuaj yeem txhim kho qhov nqus ntawm qhov ncauj thiab bioavailability ntawm LGD-4033.
Clinical Application Expansion
Ntxiv rau cov leeg nqaij atrophy thiab osteoporosis, lub peev xwm ntawm LGD-4033 nyob rau hauv cov kab mob obstructive pulmonary (COPD), lub plawv tsis ua hauj lwm, thiab lwm yam. Yuav tsum muaj kev sim tshuaj ntau ntxiv los txheeb xyuas nws txoj kev nyab xeeb thiab kev ua tau zoo yav tom ntej.
analytical Methods thiab validation
Kev txiav txim siab txog cov ntsiab lus
HPLC txoj kev: Siv C18 chromatographic kem, nrog acetonitrile- dej (muaj 0.1% formic acid) raws li theem ntawm lub xov tooj ntawm tes, ntawm tus nqi ntws ntawm 1.0 mL / min, thiab qhov ntsuas wavelength ntawm 210 nm. Txoj kev no tuaj yeem txiav txim siab cov ntsiab lus ntawmLigandrol (LGD-4033 Capsule), nrog cov kab ntau ntawm 0.1-100 ug / mL, thiab tus nqi rov qab ntawm 98% -102%.
UV-Vis spectrophotometric: Ntsuas qhov nqus ntawm 245 nm wavelength, haum rau kev tshuaj ntsuam sai. Txawm li cas los xij, kev saib xyuas yuav tsum tau them rau kev cuam tshuam ntawm excipients, thiab kev kho yuav tsum tau ua los ntawm cov txheej txheem ntxiv.
Kev tshuaj xyuas kab mob
HPLC-DAD txoj kev: Saib xyuas lub ultraviolet spectra ntawm impurity peaks los ntawm diode array detector (DAD) kom paub meej lub sij hawm tuav qhov sib txawv ntawm impurities thiab lub ntsiab ncov siab tshaj los yog sib npaug rau 0.5 feeb.
LC-MS txoj kev: Rau qis- theem impurities (xws li qis dua 0.1%), kev soj ntsuam zoo thiab ntau yuav tsum tau ua los ntawm kev siv kua chromatography-mass spectrometry (LC-MS) technology.
Kev txiav txim siab solubility
Basket method/Whisker method: Siv 0.1 M hydrochloric acid tov raws li qhov nruab nrab dissolution, nrog rau kev sib hloov ceev ntawm 50 rpm, cov nyiaj tawg tom qab 30 feeb yuav tsum ntau dua los yog sib npaug rau 80%. Txoj kev no tuaj yeem simulate cov txheej txheem nqus hauv lub cev thiab ntsuas qhov zoo ntawm kev npaj.
Kev kuaj microbial
Petri phaj txoj kev: Siv TSA (bacteriological agar) nruab nrab, cultivating ntawm 30-35℃rau 3-5 hnub, suav tag nrho cov kab mob suav.
Sabouraud's glucose agar nruab nrab: Siv rau pwm thiab cov poov xab kuaj pom, cog ntawm 20-25℃rau 5-7 hnub.
FAQ
Nws puas nce testosterone?
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Nws muaj kev tshem tawm ntev ib nrab -lub neej thiab koob tshuaj- qhov sib npaug ntawm qhov ntau npaum li cas.Nws kev tswj hwm tau cuam tshuam nrog koob tshuaj - nyob ntawm kev tawm tsam ntawm tag nrho cov testosterone, kev sib deev hormone-binding globulin, siab ceev lipoprotein cholesterol, thiab qib triglyceride.
Puas yog nws tshwm sim hauv kev sim tshuaj?
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Txawm tias nyob rau ntawm cov koob tshuaj tsawg, nws thiab nws cov metabolites tuaj yeem kuaj pom nrog cov qauv tsim rau ntau hnub lossis ntau lub lis piam nyob ntawm qhov ntsuas.. Lub sijhawm kuaj pom ntawm cov tshuaj ntsuam xyuas tau qhia hauv daim duab.
Cim npe nrov: ligandrol (lgd-4033 capsule), lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom