Timapiprant (sodium salt)

Timapiprant is a DP₂ receptor antagonist (K_i = 0.013 µM).¹ It is selective for DP₂ over the additional prostanoid receptors DP₁, TP, EP_1-4, FP, and IP (K_is = >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

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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).