LY3127760 | EP4 antagonist | Probechem Biochemicals

Chemical Structure : LY3127760

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LY3127760 (LY 3127760, LY-3127760)

货号: PC-20856Not For Human Use, Lab Use Only.

LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM.

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生物&药学活性

LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM.
LY3127760 shows exquisite selectivity over other EP receptors, with no detectable binding for EP1, EP2 or EP3.
LY3127760 displays an IC50 of 123 nM for inhibition of PGE2-induced TNFa reduction in an ex vivo LPS-stimulated human whole blood assay, a >10-fold increase in potency over CJ023,423 (Cat. PC-42700) in the same assay.
LY3127760 is active in the rat EP4 functional assay (rEP4 IC50 = 12 nM) and a suitable candidate for study in animal models of pain and inflammation.
LY3127760 (30 mg/kg) blocks inflammation in the rat adjuvant induced arthritis (AIA) model.

物理化学性质&存储条件

分子量	383.45
分子式	C21H25N3O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	O=C(NC1=C(C)C=C(C(O)=O)C=C1C)C2=C(C)C=CC(N3CCC(O)CC3)=N2

参考文献

1. Blanco, M. J. et al. Bioorg. Med. Chem. Lett. 26, 2303–2307 (2016).

LY3127760 (LY 3127760, LY-3127760)

生物&药学活性

物理化学性质&存储条件

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LY3127760 (LY 3127760, LY-3127760)

生物&药学活性

物理化学性质&存储条件

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