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Finasteride(MK-906)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Finasteride(MK-906)图片
CAS NO:98319-26-7
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
Finasteride (also known as MK-906) is a potent, reversible, and orally bioactive inhibitor of the rat type II 5 alpha-reductase with Ki of 10.2 nM, used in the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB). It is a medication used for the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB). Finasteride is a type II and type III 5α-reductase inhibitor that inhibits type II 5α reductase (IC50 = 65 nM). Suppresses the conversion of testosterone to dihydrotestosterone. It reduces prostatic dihydrotestosterone levels and prostate size in vivo.
理化性质和储存条件
Molecular Weight (MW)372.54
FormulaC23H36N2O2
CAS No.98319-26-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 75 mg/mL (201.3 mM)
Water:<1 mg/mL
Ethanol: 75 mg/mL (201.3 mM)
Other InfoChemical Name: (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-(tert-butyl)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide
InChi Key: DBEPLOCGEIEOCV-WSBQPABSSA-N
InChi Code: InChI=1S/C23H36N2O2/c1-21(2,3)25-20(27)17-8-7-15-14-6-9-18-23(5,13-11-19(26)24-18)16(14)10-12-22(15,17)4/h11,13-18H,6-10,12H2,1-5H3,(H,24,26)(H,25,27)/t14-,15-,16-,17+,18+,22-,23+/m0/s1
SMILES Code: C[C@]12CC[C@H]3[C@@H](CC[C@@H]4[C@]3(C)C=CC(N4)=O)[C@@H]1CC[C@@H]2C(NC(C)(C)C)=O
SynonymsMK-906; MK906; Proscar, Eucoprost, Propecia, MK 906
实验参考方法
In Vitro

In vitro activity: Finasteride binds to the type 2 isozyme-NADPH complex to form a ternary complex with Ki of 1.19 nM, which then rearranges to a high affinity complex (E:I) with a pseudo first order rate constant of 1.62 ms. Finasteride dose-dependently inhibits the growth rate of the LnCap cell line. Finasteride markedly inhibits prostate-specific antigen (PSA) secretion and expression in LNCaP cells.


Kinase Assay: Finasteride is an orally active testosterone 5-alpha-reductase inhibitor (Ki= 10 nM). Target: 5-alpha Reductase Approved: 1992 Finasteride, a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5α-reductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). Finasteride is used in the treatment of prostate cancer, benign prostatic hyperplasia, and androgenetic alopecia (male pattern baldness). In benign prostatic hyperplasia, finasteride inhibits 5alpha-reductase activity in epithelium for Ki of 10 nM, significantly lower than in stroma (Ki = 33nM).

In VivoFinasteride induces dosage-related incidences of hypospadias (penischisis) in male offspring with a threshold dosage level near 0.1 mg/kg/day and a 100% effect level of 100 mg/kg/day in male rats. Finasteride also causes decreased anogenital distance in male offspring in male rats. Finasteride and castration decreases prostate weight at day 21 by 65% and 93%, respectively, in rats. Finasteride has no significant effect on DNA content after 4 days and decreases DNA content by a maximum of 52% at 14 days in rats. Finasteride causes a less intense increase in staining in which 16% of epithelial cells stained for tissue transglutaminase on day 9 with a return to baseline by day 14 in rats. Finasteride-induced staining is less intense with peak staining at day 4 (0.7% of epithelial cells) and a return to control values by day 9 in rats.
Animal modelRats
Formulation & Dosage0.1 mg/kg; 100 mg/kg
ReferencesJ Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64; Teratology. 1990 Jul;42(1):91-100.