GSK-2881078
Based on 5 publication(s) in Google Scholar
GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.42%
- CAS 番号: 1539314-06-1
- 分子式: C14H13F3N2O2S
- 分子量:330.33
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 GSK-2881078
More- Drug Test Anal. 2022 Feb;14(2):349-370. [Abstract]
- Drug Test Anal. 2021 May;13(5):916-928. [Abstract]
- Drug Test Anal. 2021 Feb;13(2):283-298. [Abstract]
- J Steroid Biochem Mol Biol. 2019 May:189:81-86. [Abstract]
- Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2026 Feb 26:1-17. [Abstract]
生物活性
GSK-2881078 has EC50s of 4.44 μM and 3.99 × 10−3 μM for reporter gene of androgen inducible yeast and PC3(AR)2 cells (human prostate carcinoma cell), respectively[4].
GSK-2881078 (10−5-10 μM, 24 h) stimulates reporter gene expression dose-dependently in the PC3(AR)2, increasing the relative luminescence units from 140% to 17340%[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1539314-06-1
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性状 Solid
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分子量 330.33
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分子式 C14H13F3N2O2S
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Color White to off-white
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SMILES
N#CC1=C(C(F)(F)F)C2=C(N([C@H](C)CS(=O)(C)=O)C=C2)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Drug Test Anal
Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes. [Abstract]2022 Feb;14(2):349-370. PMID: 34714606 -
Drug Test Anal
An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile. [Abstract]2021 May;13(5):916-928. PMID: 33283964 -
Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861 -
J Steroid Biochem Mol Biol
Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay. [Abstract]2019 May:189:81-86. PMID: 30825507 -
Food Addit Contam Part A Chem Anal Control Expo Risk Assess
Comprehensive IM-MS approach for SARMs detection in urine: building CCS databases to support food safety monitoring. [Abstract]2026 Feb 26:1-17. PMID: 41747154
溶剤 & 溶解度
DMSO : ≥ 33 mg/mL (99.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Xie Y, et al. Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021). Eur J Med Chem. 2022;230:114119. [Content Brief]
[2]. Clark RV, et al. Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women. Br J Clin Pharmacol. 2017 Oct;83(10):2179-2194. [Content Brief]
[3]. Neil D, et al. GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women. J Clin Endocrinol Metab. 2018;103(9):3215-3224. [Content Brief]
[4]. Zierau O, et al. Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay. J Steroid Biochem Mol Biol. 2019 May;189:81-86. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0273 mL | 15.1364 mL | 30.2728 mL | 75.6819 mL |
| 5 mM | 0.6055 mL | 3.0273 mL | 6.0546 mL | 15.1364 mL | |
| 10 mM | 0.3027 mL | 1.5136 mL | 3.0273 mL | 7.5682 mL | |
| 15 mM | 0.2018 mL | 1.0091 mL | 2.0182 mL | 5.0455 mL | |
| 20 mM | 0.1514 mL | 0.7568 mL | 1.5136 mL | 3.7841 mL | |
| 25 mM | 0.1211 mL | 0.6055 mL | 1.2109 mL | 3.0273 mL | |
| 30 mM | 0.1009 mL | 0.5045 mL | 1.0091 mL | 2.5227 mL | |
| 40 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8920 mL | |
| 50 mM | 0.0605 mL | 0.3027 mL | 0.6055 mL | 1.5136 mL | |
| 60 mM | 0.0505 mL | 0.2523 mL | 0.5045 mL | 1.2614 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL |
GSK-2881078 関連分類
HY-100186 関連分類
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