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GSK-2881078

GSK-2881078

Item no.	HY-100186-2mg
Manufacturer	MedChem Express
CASRN	1539314-06-1
Amount	2 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 1 mg 25 mg 2 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.74
Citations	[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.\|[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.\|[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.\|[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.
Smiles	N#CC1=C(C(F)(F)F)C2=C(N([C@H](C)CS(=O)(C)=O)C=C2)C=C1
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1539314-06-1
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Neuroscience-Neuromodulation
Manufacturer - Targets	Androgen Receptor
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	330.33
Product Description	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[1][2][3][4].
Manufacturer - Research Area	Cancer; Endocrinology; Metabolic Disease; Inflammation/Immunology; Cardiovascular Disease; Others
Solubility	DMSO: ≥ 33 mg/mL
Manufacturer - Pathway	Vitamin D Related/Nuclear Receptor
Clinical information	Phase 2

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

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HY-100186-2mg-safety-datasheet.pdf