BMS-986278

BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases In Vitro BMS-986278 is a high-affinity LPA1 antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1 in CHO cells overexpressing LPA1. BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a K b of 5.8 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo BMS-986278 (0.1-10 mg/kg; a single p.o.) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner in CD1 mice . BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats . Pharmacokinetics of BMS-986278 in preclinical species plasma clearance ((mL/min)/kg) V ss (L/kg) oral bioavailability (%) T 1/2 (h) plasma protein binding (% free) mouse 37 5.5 70 2.5 31.4 rat 15 3.5 100 4.5 12.6 monkey 2.0 1.6 79 11 0.8 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (10 weeks) were administered Bleomycin Dosage: 3, 10, and 30 mg/kg Administration: P.o. twice daily for 14 days Result: Resulted in significant decreases in the lung section percent fibrotic area for the 3 mg/kg (48%) and 10 mg/kg (56%) dose groups. Form:Solid IC50& Target:Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1)

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