CAY10471

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^[1][2][3]. IC50 & Target:IC50: CRTH2^[1] In Vitro: CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells^[1].
In Vivo: 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^[2].
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)^[3].