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GPR31 antagonist SAH2

Chemical Structure : GPR31 antagonist SAH2

CAS No.: 58116-43-1

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GPR31 antagonist SAH2 (SLU-0011371, SAH2)

Catalog No.: PC-21741Not For Human Use, Lab Use Only.

GPR31 antagonist SAH2 (SLU-0011371) is the first highly potent and selective small molecule GPR31 antagonist, antagonizes 12(S)-HETE-induced β-arrestin recruitment with IC50 of 1.09 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GPR31 antagonist SAH2 (SLU-0011371) is the first highly potent and selective small molecule GPR31 antagonist, antagonizes 12(S)-HETE-induced β-arrestin recruitment with IC50 of 1.09 uM.
GPR31 antagonist SAH2 (SLU-0011371) binds to hydrophobic pocket and its carboxylic acid can interact with R98 in transmembrane domain (TM) 3 and R242 in TM5.
SAH2 (10 mg/kg, intrathecal injection) reverse CCI-induced behavioral hypersensitivities in male and female mice.

Physicochemical Properties

M.Wt 403.52
Formula C23H33NO5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((((10R,13S,17R,E)-17-acetyl-17-hydroxy-10,13-dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-ylidene)amino)oxy)acetic acid

References

1. Giancotti LA, et al. J Pharmacol Exp Ther. 2024 Jan 26:JPET-AR-2023-001853.

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