| Bioactivity | 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]. |
| Target | IC50: CRTH2 |
| Invitro | CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells[1]. Western Blot Analysis[1] Cell Line: |
| 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]. Animal Model: |
| Name | CAY10471 |
| CAS | 627865-18-3 |
| Formula | C21H21FN2O4S |
| Molar Mass | 416.47 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Hatanaka M, et al. 15d-prostaglandin J2 enhancement of nerve growth factor-induced neurite outgrowth is blocked by the chemoattractant receptor- homologous molecule expressed on T-helper type 2 cells (CRTH2) antagonist CAY10471 in PC12 cells. J Pharmacol [2]. Matsushima Y, et al. Distinct roles of prostaglandin D2 receptors in chronic skin inflammation.Mol Immunol. 2011 Oct;49(1-2):304-10. [3]. Ito H, et al. PGD2-CRTH2 pathway promotes tubulointerstitial fibrosis.J Am Soc Nephrol. 2012 Nov;23(11):1797-809. |
CAY10471
CAS: 627865-18-3 F: C21H21FN2O4S W: 416.47
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 atten
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