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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-Setipiprant
Setipiprant

Chemical Structure : Setipiprant

CAS No.: 866460-33-5

Setipiprant (ACT-129968, KYTH-105, ACT129968)

货号: PC-20092Not For Human Use, Lab Use Only.

Setipiprant (ACT-129968, KYTH-105) is a potent, selective and orally available CRTH2 antagonist with IC50 of 6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Setipiprant (ACT-129968, KYTH-105) is a potent, selective and orally available CRTH2 antagonist with IC50 of 6 nM.
Setipiprant is selective for CRTH2/DP2 over DP1 in a radioligand binding assay (IC50=1,290 nM) and the prostaglandin E2 receptor subtypes EP2 and EP4 in a β-arrestin assay (IC50s=2,600 and >10,000 nM, respectively).
Setipiprant inhibited PGD2-induced calcium flux in HEK293 cells expressing human CRTH2/DP2 (IC50 = 30 nM) and PGD2-induced shape change in human eosinophils (IC50=235 nM).
Setipiprant reduced both the allergen-induced LAR and the associated AHR in allergic asthmatics.

物理化学性质&存储条件

分子量 402.43
分子式 C24H19FN2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid

参考文献

1. Risch P, et al. J Med Chem. 2015 Oct 22;58(20):8011-35.

2. Diamant Z, et al. Clin Exp Allergy. 2014 Aug;44(8):1044-52.

3. Fretz H, et al. J Med Chem. 2013 Jun 27;56(12):4899-911.

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