| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Epristeride targets the enzyme steroid 5 alpha-reductase type 2 (SR isoenzyme 2), which converts testosterone to the more potent androgen dihydrotestosterone (DHT). It acts as a potent uncompetitive inhibitor of this enzyme. While it is a strong inhibitor of the type 2 isoenzyme, it exhibits weak inhibitory effects on the type 1 isoenzyme. By inhibiting 5α-reductase type 2, Epristeride reduces the production of DHT in target tissues such as the prostate and skin, thereby modulating androgen-dependent processes.
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| ln Vitro |
Epristeride blocks SR isoenzyme type 2 (SR2) with a Ki value of 0.7–2 nM[1].
Epristeride demonstrates potent in vitro inhibitory effects on steroid 5 alpha-reductase isoenzyme type 2, with a Ki value of 0.7-2 nM. The compound's uncompetitive inhibition mechanism means it binds to the enzyme-substrate complex rather than the free enzyme. As a selective inhibitor of the type 2 isoenzyme, it shows much weaker activity against the type 1 isoenzyme, indicating a high degree of selectivity for the target. This selectivity profile makes it useful for studying the specific role of the type 2 isoenzyme in androgen physiology. |
| ln Vivo |
Epristeride is an orally active compound with demonstrated efficacy in animal models of androgen-dependent conditions. Its oral bioavailability allows for convenient administration in preclinical studies. In vivo, Epristeride effectively reduces DHT levels in target tissues by inhibiting the 5α-reductase type 2 enzyme. It has been studied for its effects on prostate size and androgen-driven processes. The compound is used in research models of benign prostatic hyperplasia to evaluate its potential to reduce prostate growth and improve urinary function.
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| Enzyme Assay |
The 5α-reductase enzyme inhibition assay typically involves incubating the test compound with human or rat prostatic microsomes as a source of 5α-reductase enzyme. The reaction mixture contains [¹⁴C]-testosterone as substrate and NADPH as a cofactor. Epristeride is added at various concentrations, and the reaction is carried out at 37°C for a specified time. The reaction is terminated by extraction with organic solvent, and the production of [¹⁴C]-DHT is quantified by thin-layer chromatography or HPLC followed by scintillation counting. Ki values are calculated from the inhibition curves.
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| Cell Assay |
For evaluating the cellular effects of Epristeride, human prostate epithelial or stromal cells can be cultured in vitro and treated with varying concentrations of the compound. The cells are maintained in appropriate medium supplemented with fetal bovine serum. After treatment, the production of DHT from testosterone is measured in the cell culture medium using ELISA or LC-MS/MS. Alternatively, the compound's effect on androgen-responsive gene expression can be assessed by quantitative PCR. Cell viability is monitored using standard assays such as MTT to ensure that observed effects are not due to cytotoxicity.
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| Animal Protocol |
To evaluate the in vivo efficacy of Epristeride, male rats are typically used as an animal model. Animals are orally administered Epristeride at various doses (e.g., 1-30 mg/kg) once daily for a period of 2-4 weeks. At the end of the treatment period, animals are euthanized, and prostate tissue is collected and weighed. Blood samples are collected for measurement of serum DHT and testosterone levels. The prostate weight reduction and changes in DHT levels are measured as indicators of 5α-reductase inhibition. Efficacy is expressed as the percentage reduction in prostate weight and DHT levels relative to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Epristeride is characterized as being orally bioavailable, allowing for effective administration via the oral route in animal models. While specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources, its oral activity and efficacy in in vivo models confirm adequate systemic exposure. The compound's molecular weight of 399.57 and lipophilic nature are consistent with good oral absorption characteristics typical of steroid-like molecules.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Epristeride are not provided in the available sources. As a research compound intended for laboratory use, its safety profile has likely been evaluated in standard preclinical toxicology studies. The compound is not approved for human therapeutic use and is intended for research applications only. Standard safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment.
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| References | |
| Additional Infomation |
Epristeride is a steroidal acid.
Epristeride is also known as ONO-9302 and SKF105657. Its IUPAC name is (8S,9S,10R,13S,14S,17S)-17-(tert-butylcarbamoyl)-10,13-dimethyl-2,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3-carboxylic acid. The compound is a selective and specific inhibitor of human steroid 5 alpha-reductase isoform 2 and is used for research on benign prostatic hyperplasia and acne. It is supplied for research purposes only with a purity of ≥98%. |
| Molecular Formula |
C₂₅H₃₇NO₃
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| Molecular Weight |
399.57
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| Exact Mass |
399.277
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| CAS # |
119169-78-7
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| Related CAS # |
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| PubChem CID |
68741
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| Appearance |
White to off-white solid powder
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| Density |
1.13g/cm3
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| Boiling Point |
596ºC at 760mmHg
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| Melting Point |
242-249°
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| Flash Point |
314.3ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.563
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| LogP |
5.491
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
788
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)NC(C)(C)C)CC=C4[C@@]3(CCC(=C4)C(=O)O)C
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| InChi Key |
VAPSMQAHNAZRKC-PQWRYPMOSA-N
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| InChi Code |
InChI=1S/C25H37NO3/c1-23(2,3)26-21(27)20-9-8-18-17-7-6-16-14-15(22(28)29)10-12-24(16,4)19(17)11-13-25(18,20)5/h6,14,17-20H,7-13H2,1-5H3,(H,26,27)(H,28,29)/t17-,18-,19-,20+,24-,25-/m0/s1
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| Chemical Name |
17β-(tert-Butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
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| Synonyms |
ONO-9302; SKF-105657; ONO9302; SKF105657; ONO 9302; SKF 105657; Brand name in China: Aipuliete and Chuanliu
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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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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5027 mL | 12.5135 mL | 25.0269 mL | |
| 5 mM | 0.5005 mL | 2.5027 mL | 5.0054 mL | |
| 10 mM | 0.2503 mL | 1.2513 mL | 2.5027 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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