CAS NO: | 98319-26-7 |
规格: | ≥98% |
包装 | 价格(元) |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
Molecular Weight (MW) | 372.54 |
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Formula | C23H36N2O2 |
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 Info | Chemical 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 |
Synonyms | MK-906; MK906; Proscar, Eucoprost, Propecia, MK 906 |
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). |
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In Vivo | Finasteride 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 model | Rats |
Formulation & Dosage | 0.1 mg/kg; 100 mg/kg |
References | J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64; Teratology. 1990 Jul;42(1):91-100. |