GPR183 antagonist 32

Chemical Structure : GPR183 antagonist 32

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货号: PC-21501Not For Human Use, Lab Use Only.

GPR183 antagonist 32 is potent, selective antagonist of GPR183 (EBI2) with IC50 of 8.6/12.1 nM (human/mouse β-arrestin), respectively.

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200 mg		Get quote

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生物&药学活性

GPR183 antagonist 32 is potent, selective antagonist of GPR183 (EBI2) with IC50 of 8.6/12.1 nM (human/mouse β-arrestin), respectively.
GPR183 antagonist 32 blocks human U937 and Th17 cell migration with IC50 values of 5.5 nM and 3.8 nM, respectively.
GPR183 antagonist 32 does not show any cytotoxicity to human hepatocytes, with an IC50 value of more than 150 μM.
GPR183 antagonist 32 potently antagonizes 7α,25-OHC-induced calcium mobilization in vitro (IC50=31.3 nM).
GPR183 antagonist 32 (0.1, 0.3, and 1.0 mg/kg) reduced inflammation, bone erosion, pannus formation, and cartilage damage, downregulated the expression of multiple CIA-associated genes in the paw joints of CIA mice.

物理化学性质&存储条件

分子量	432.38
分子式	C20H18F2N4O5
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	(E)-3-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-1-(4-(2-methoxypyrimidine-5-carbonyl)piperazin-1-yl)prop-2-en-1-one

参考文献

1. Francois Gessier, et al. J Med Chem. 2014 Apr 24;57(8):3358-68.