BMS-986278

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-986278 是一种有效和具有口服活性的血磷脂酸受体 1 (LPA1) 拮抗剂，对人和小鼠 LPA1 的 Kb 值分别为 6.9 nM 和 4.0 nM。BMS-986278 可用于研究肺纤维化疾病。

BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs 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.

BMS-986278 is a high-affinity LPA1 antagonist, with Kbs 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 Kb of 5.8 nM.

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.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.

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GPCR/G Protein

LPA Receptor

LPA Receptor

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2170126-74-4

445.51

C22H31N5O5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (224.46 mM; 超声助溶 )

CCCN(C)C(=O)OCc1c(nnn1C)-c1ccc(O[C@H]2CCC[C@@H](C2)C(O)=O)c(C)n1

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(-20℃)

With Ice Pack

≥ 2 years