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Chemical Structure : Setipiprant
CAS No.: 866460-33-5
Catalog No.: 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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|---|---|---|---|
| 25 mg | $228 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | $688 | In stock | |
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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.
| M.Wt | 402.43 | |
| Formula | C24H19FN2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid |
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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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