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GPR54 antagonist 15a

Chemical Structure : GPR54 antagonist 15a

CAS No.: 925924-27-2

GPR54 antagonist 15a

Catalog No.: PC-21175Not For Human Use, Lab Use Only.

GPR54 antagonist 15a is a potent, selective, small molecule antagonist of GPR54 with IC50 of 3.6/15 nM (human/rat GPR54) in receptor binding assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GPR54 antagonist 15a is a potent, selective, small molecule antagonist of GPR54 with IC50 of 3.6/15 nM (human/rat GPR54) in receptor binding assays.
GPR54 antagonist 15a exhibits fully potent antagonist activity (IC50=0.93 μM) in cellular Ca2+ mobilization assays.
GPR54 antagonist 15a (0.22 mg/kg, i.v.) suppressed the plasma luteinizing hormone (LH) level in castrated male rats.

Physicochemical Properties

M.Wt 519.96
Formula C27H23ClFN5O3
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

N-[3-Cyano-6-(4-fluoro-2-hydroxyphenyl)-4-(3-piperazin-1-ylphenyl)pyridin-2-yl]furan-2-carboxamide hydrochloride

References

1. Kobayashi T, et al. Bioorg Med Chem. 2010 Jul 15;18(14):5157-71.

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