An antagonist of CRTH2/DP2
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Setipiprant

Item No. 28291

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-fluoro-1,2,3,4-tetrahydro-2-(1-naphthalenylcarbonyl)-5H-pyrido[4,3-b]indole-5-acetic acid
CAS Number
866460-33-5
Synonyms
  • ACT-129968
Molecular Formula
C24H19FN2O3
Formula Weight
402.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 30 mg/mlEthanol: 3 mg/ml
λmax
224, 283 nm
SMILES
O=C(C1=CC=CC2=C1C=CC=C2)N3CC4=C(N(CC(O)=O)C5=C4C=C(F)C=C5)CC3
InChi Code
InChI=1S/C24H19FN2O3/c25-16-8-9-21-19(12-16)20-13-26(11-10-22(20)27(21)14-23(28)29)24(30)18-7-3-5-15-4-1-2-6-17(15)18/h1-9,12H,10-11,13-14H2,(H,28,29)
InChi Key
IHAXLPDVOWLUOS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $102

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    50 mg

    $418

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    100 mg

    $627

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    Product Description

    Setipiprant is an orally bioavailable antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (IC50 = 6 nM for the human receptor).1 It is selective for CRTH2/DP2 over DP1 in a radioligand binding assay (IC50 = 1,290 nM) and the prostaglandin E2 (PGE2; Item No. 14010) receptor subtypes EP2 and EP4 in a β-arrestin assay (IC50s = 2,600 and >10,000 nM, respectively). Setipiprant inhibits 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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fretz, H., Valdenaire, A., Pothier, J., et al. Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist. J. Med. Chem. 56(12), 4899-4911 (2013).