A DP2 receptor antagonist
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Timapiprant (sodium salt)

Item No. 42734

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-2-methyl-3-(2-quinolinylmethyl)-1H-indole-1-acetic acid, monosodium salt
CAS Number
950688-14-9
Synonyms
  • OC000459
Molecular Formula
C21H16FN2O2 • Na
Formula Weight
370.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/mlPBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml
SMILES
CC1=C(CC2=NC3=C(C=CC=C3)C=C2)C4=C(C=CC(F)=C4)N1CC([O-])=O.[Na+]
InChi Code
InChI=1S/C21H17FN2O2.Na/c1-13-17(11-16-8-6-14-4-2-3-5-19(14)23-16)18-10-15(22)7-9-20(18)24(13)12-21(25)26;/h2-10H,11-12H2,1H3,(H,25,26);/q;+1/p-1
InChi Key
XKRNYIKRDAGPQZ-UHFFFAOYSA-M
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

    $97

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    25 mg

    $203

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    Product Description

    Timapiprant is a DP2 receptor antagonist (Ki = 0.013 µM).1 It is selective for DP2 over the additional prostanoid receptors DP1, TP, EP1-4, FP, and IP (Kis = >10 µM for all). Timapiprant inhibits calcium mobilization induced by prostaglandin D2 (PGD2; Item No. 12010) in CHO cells expressing human DP2 (IC50 = 0.028 µM). It inhibits PGD2-induced Th2 T helper cell chemotaxis, IL-13 production, and apoptosis (IC50s = 0.028, 0.019, and 0.035 µM, respectively). In vivo, timapiprant reduces PGD2-induced blood eosinophilia in rats (ED50 = 0.04 mg/kg) and pulmonary eosinophil accumulation in guinea pigs (ED50 = 0.01 mg/kg). It also reduces amyloid-β (Aβ) plaque area and hippocampal microglial accumulation and improves learning and memory deficits in the TgF344 transgenic rat model of age-dependent and progressive Alzheimer’s disease.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pettipher, R., Vinall, S.L., Xue, L., et al. Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. J. Pharmacol. Exp. Ther. 340(2), 473-482 (2012).

    2. Wallace, C.H., Oliveros, G., Serrano, P.A., et al. Timapiprant, a prostaglandin D2 receptor antagonist, ameliorates pathology in a rat Alzheimer’s model. Life Sci. Alliance 5(12), e202201555 (2022).