BI-671800

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI-671800 是 Th2 细胞 (DP2/CRTH2) 上趋化剂受体同源分子的高度特异性和有效的拮抗剂。

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 potential for the treatment of poorly controlled asthma.

BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells.

BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice. BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals. Animal Model:6-8-week-old age- and sex-matched BALB/c mice (mice were sensitized for 14 days, challenged intranasally).Dosage:10-0.1 mg/kg Administration:Oral gavage for 4 weeks Result:Shows significant inhibition of AHR in mice.

AP-761 | Cmpd A

Cell Cycle/DNA Damage

GPR

CRTh2 (DP2) receptor|hCRTH2|mCRTH2

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1093108-50-9

501.5

C25H26F3N5O3

>98% (HPLC)

DMSO:130 mg/mL (259.22 mM; Need ultrasonic)

CN(C)c1nc(Cc(cc2)ccc2NC(c2ccc(C(F)(F)F)cc2)=O)nc(N(C)C)c1CC(O)=O

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(-20℃)

With Ice Pack

≥ 2 years