产品
编 号:F410278
分子式:C21H21FN2O4S
分子量:416.47
产品类型
结构图
CAS No: 627865-18-3
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产品详情
生物活性:
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2?antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.
体内研究:
CAY10471 (oral treatment; 2 mg/kg; challenged on day 22 or over 10 consecutive days) shows a diminished inflammation in chronic contact hypersensitivity (CHS) and IgE-CAI model. It blocks CRTH2 partly, but significantly suppresses inflammation in mice.CAY10471 (oral adminstration; 20 mg/kg; twice daily; beginning 3/4/5 days before UUO) significantly attenuates interstitial collagen deposition in the cortex when compared with the vehicle (8.40% versus 14.85%). Oral administration from 3 days after UUO also significantly attenuates interstitial collagen deposition in the cortex compared with vehicle (9.63% versus 14.44%). However, oral administration beginning 5 days after UUO has little effect on interstitial collagen deposition in the cortex when compared with vehicle (14.61% versus 15.09%). Unilateral ureteral obstruction (UUO).Animal Model:Balb/c mice, DP?/? mice, CRTH2?/? mice
Dosage:2 mg/kg
Administration:Oral treatment; once daily; challenged on day 22 or over 10 consecutive days
Result:Significantly suppressed both CHS and IgE-CAI inflammatory responses.
Animal Model:C57BL/6 mice
Dosage:20 mg/kg
Administration:Oral treatment; twice daily; beginning 3/4/5 days before UUO
Result:Slowed the progression of renal fibrosis in the obstructed kidneys.
体外研究:
CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells.