产品
编 号:F052499
分子式:C24H22N2O5S2
分子量:482.57
产品类型
结构图
CAS No: 1164500-72-4
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产品详情
生物活性:
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.
体外研究:
ML 145 (10 μM) also fully blocks internalization of human FLAG-GPR35-eYFP in response to varying concentrations of Zaprinast, Cromolyn disodium, and Pamoate. ML 145 is either without effect (mouse) or displays only a small and apparently noncompetitive inhibitory effect (rat) at the rodent orthologs. ML 145 acts as a competitive antagonist for a number of agonists at human GPR35 and has an IC50 value against EC80 concentrations of various GPR35 agonists in the region of 20 nM.