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Purity: ≥98%
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.
| Targets |
Type II 5α-reductase （IC50: 4.2 nM)
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| ln Vitro |
In PC-3 cells, finasteride (10 μM; 6–24 h) stimulates the expression of the proteins Nrf2 and HO-1[2]. Finasteride inhibits P. crustosum's ability to convert [3H]testosterone (T) to [3H]dihydrotestosterone (DHT)[1].
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| ln Vivo |
In dogs with BPH, finasteride (0.1–0.5 mg/kg; po once daily for 16 weeks) lowers prostatic size without negatively impacting the quality of the semen or the level of serum testosterone[3].
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| Enzyme Assay |
In order to develop the treatment for 5α-DHT associated diseases such as BPH and PCa, a simple test system has been required to screen for 5α-SR inhibitors. Because of its simplicity and high sensitivity, the present method is also applicable to the simple test system for screening 5α-SR inhibitors. After confirming that finasteride showed no effect on the enzyme cycling of 5α-DHT, we performed the inhibition experiments by finasteride of rat liver and prostate microsomal 5α-SR. From the results, the concentrations of finasteride required to inhibit 5α-SR activity by 50% (IC50) were estimated to be 21 nM for liver 5α-SR and 20 nM for prostate 5α-SR, respectively. The inhibitions of rat 5α-SR1 and 5α-SR2 by fenasteride have been investigated by using COS cells transiently expressing 5α-SR1 and 5α-SR2. The IC50 values of finasteride to 5α-SR1 and 5α-SR2 were evaluated to be and 5.2 nM respectively in whole cell assay, whereas those were 13 and 1.0 nM respectively in the assay with crude enzyme preparations.21 The IC50 value of finasteride to rat 5α-SR in prostate microsomes was also evaluated to be 11 nM by Häusler et al., 13 nM by Igarashi et al. and 237 nM by Mitamura et al. The reported IC50 values of fenasteride to rat 5α-SR in prostate homogenate were in the range from 6.8 to 147 nM. The reason for such a difference may be related to differences in experimental conditions of enzyme activity evaluation such as pH, testosterone concentration and enzyme preparation[4].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: PC-3, DU-145, and LNCaP cells Tested Concentrations: 10 μM Incubation Duration: 6, 12, 24 h Experimental Results: Increased the expression of HO-1 protein in a time-dependent manner in PC-3 cells. Induced the expression of Nrf2 protein in DU-145 and PC-3 cells, but not in LNCaP cells. |
| Animal Protocol |
Animal/Disease Models: Male dogs with spontaneous BPH (2.7-11 years old ; 10.3-49 kg)[3]
Doses: 0.1-0.5 mg/kg Route of Administration: Po one time/day for 16 weeks Experimental Results: diminished prostatic diameter (20%), prostatic volume (43%), and serum DHT concentration (58%) . diminished semen volume but did not adversely effect on semen quality or serum testosterone concentration. No adverse effects on dogs. |
| References |
[1]. Flores E, et, al. Steroid 5alpha-reductase inhibitors. Mini Rev Med Chem. 2003 May;3(3):225-37.
[2]. Yun DK, et, al. Finasteride Increases the Expression of Hemoxygenase-1 (HO-1) and NF-E2-Related Factor-2 (Nrf2) Proteins in PC-3 Cells: Implication of Finasteride-Mediated High-Grade Prostate Tumor Occurrence. Biomol Ther (Seoul). 2013 Jan;21(1):49-53. [3]. Sirinarumitr K, et, al. Effects of finasteride on size of the prostate gland and semen quality in dogs with benign prostatic hypertrophy. J Am Vet Med Assoc. 2001 Apr 15;218(8):1275-80. [4]. Spectrophotometric method for the assay of steroid 5α-reductase activity of rat liver and prostate microsomes. Anal Sci. 2013;29(4):455-9. doi: 10.2116/analsci.29.455. |
| Molecular Formula |
C23H36N2O2
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|---|---|---|
| Molecular Weight |
372.54
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| Exact Mass |
372.2776
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| Elemental Analysis |
C, 74.15; H, 9.74; N, 7.52; O, 8.59
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| CAS # |
98319-26-7
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| Related CAS # |
Finasteride acetate;222989-99-3;Finasteride-d9;1131342-85-2
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| Appearance |
White to off-white solid powder
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| LogP |
3
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| tPSA |
58.2Ų
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| SMILES |
O=C([C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])[C@]4([H])[C@@](C([H])=C([H])C(N4[H])=O)(C([H])([H])[H])[C@@]3([H])C([H])([H])C([H])([H])[C@@]21C([H])([H])[H])N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
DBEPLOCGEIEOCV-WSBQPABSSA-N
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| 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
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| 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
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6843 mL | 13.4214 mL | 26.8428 mL | |
| 5 mM | 0.5369 mL | 2.6843 mL | 5.3686 mL | |
| 10 mM | 0.2684 mL | 1.3421 mL | 2.6843 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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