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GSK-2881078

CAT: 0804-HY-100186-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-100186-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
1539314-06-1
UNSPSC
12352005
Hazard Statement
H301, H360
Target
Androgen Receptor
Type
Reference compound
Related Pathways
Vitamin D Related/Nuclear Receptor
Applications
Neuroscience-Neuromodulation
Field of Research
Cancer; Endocrinology; Metabolic Disease; Inflammation/Immunology; Cardiovascular Disease; Others
Assay Protocol
https://www.medchemexpress.com/GSK-2881078.html
Purity
99.42
Solubility
DMSO : ≥ 33 mg/mL
Smiles
N#CC1=C(C(F)(F)F)C2=C(N([C@H](C)CS(=O)(C)=O)C=C2)C=C1
Molecular Formula
C14H13F3N2O2S
Molecular Weight
330.33
Precautions
H301, H360
References & 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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2

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