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产品介绍
产品介绍
产品信息
商品描述
BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.
分子量
445.51
可溶性
DMSO:90 mg/mL (202.02 mM)
In vitro(体外研究)
With Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, BMS-986278 is a high-affinity LPA1 antagonist. These values were determined in CHO cells overexpressing LPA1[1]. BMS-986278 also antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, exhibiting a Kb of 5.8 nM[1].
In vivo(体内研究)
In CD1 mice, a single oral administration of BMS-986278 (0.1-10 mg/kg) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner[1]. Furthermore, when administered orally twice daily for 14 days at doses ranging from 3 to 30 mg/kg, BMS-986278 reduces Bleomycin-induced collagen deposition and lung fibrosis in rats[1].
背景
分子式
C22H31N5O5
CAS号
2170126-74-4
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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