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CAY10471
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAY10471图片
CAS NO:627865-18-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
TM30089
产品介绍
CAY10471 (TM30089) 是一种强效、选择性和具有口服活性的前列腺素 D2 受体CRTH拮抗剂。CAY10471 在动物模型中,减缓小管间质纤维化和慢性接触性超敏反应 (CHS) 的进程。
生物活性

CAY10471 (TM30089) is a potent, selective, and orally activeprostaglandin 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]

体外研究
(In Vitro)

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:PC12 cells
Concentration:1 μM
Incubation Time:1 or 24 hours
Result:Blocked 15d-PGJ2-induced p38 MAP kinase activation.
体内研究
(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:Balb/c mice, DP–/–mice, CRTH2–/–mice[2]
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[3]
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.
分子量

416.47

Formula

C21H21FN2O4S

CAS 号

627865-18-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.