product name Finasteride
Description: Finasteride (also known as MK-906) is a potent, reversible, orally active 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.
References: J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64; Teratology. 1990 Jul;42(1):91-100.
372.54
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)
Solubility (In vivo)
Synonyms
MK-906
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399834
| 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: Cell Assay: |
|---|---|
| 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 | |
| Formulation & Dosage | |
| References | J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64; Teratology. 1990 Jul;42(1):91-100. |
Related Posts
product name Finasteride
Description: Finasteride (also known as MK-906) is a potent, reversible, orally active 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.
References: J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64; Teratology. 1990 Jul;42(1):91-100.
372.54
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)
Solubility (In vivo)
Synonyms
MK-906
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399834
| 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: Cell Assay: |
|---|---|
| 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 | |
| Formulation & Dosage | |
| References | J Steroid Biochem Mol Biol. 1997 Apr;61(1-2):55-64; Teratology. 1990 Jul;42(1):91-100. |