Timapiprant (sodium salt)

Timapiprant is a DP2 receptor antagonist (Ki = 0. µM). 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, Cay-12010) in CHO cells expressing human DP2 (IC50 = 0. µM). It inhibits PGD2-induced Th2 T helper cell chemotaxis, IL-13 production, and apoptosis (IC50s = 0. 0. and 0. µM, respectively). In vivo, timapiprant reduces PGD2-induced blood eosinophilia in rats (ED50 = 0. mg/kg) and pulmonary eosinophil accumulation in guinea pigs (ED50 = 0. mg/kg). It also reduces amyloid-beta (Abeta) 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.. Solulibility: DMSO: Sparingly soluble: 1-10 mg/ml: Ethanol: Slightly soluble: 0.1-1 mg/ml, PBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml.