产品
编 号：F762394
分子式：C22H31N5O5
分子量：445.51
分子式：C22H31N5O5
分子量：445.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2170126-74-4
产品详情
生物活性：
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.
体内研究：
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 speciesplasma clearance ((mL/min)/kg) Vss (L/kg) oral bioavailability (%) T1/2 (h) plasma protein binding (% free)
mouse375.5702.531.4
rat153.51004.512.6
monkey2.01.679110.8
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.
体外研究：
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 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.
体内研究：
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 speciesplasma clearance ((mL/min)/kg) Vss (L/kg) oral bioavailability (%) T1/2 (h) plasma protein binding (% free)
mouse375.5702.531.4
rat153.51004.512.6
monkey2.01.679110.8
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.
体外研究：
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.
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