BI-671800 是高特异性的前列腺素 D2 受体拮抗剂,对哮喘有研究潜力,对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。
产品描述
BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2). With IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has the potential to treat poorly controlled asthma[2].
体外活性
BI-671800 (compound A) exhibits low nM potency as a potent small-molecule antagonist of human or mouse CRTH2 in transfected cells[1].
体内活性
BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice[1]. BI-671800 (compound A) also effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals[3].
Cas No.
1093108-50-9
分子式
C25H26F3N5O3
分子量
501.5
别名
Cmpd A;AP-761
储存和溶解度
DMSO:130 mg/mL (259.22 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years