BMS-986278 |
| Catalog No.GC63895 |
BMS-986278 is an orally active, high-affinity and potent small molecule LPA1 antagonist that is commonly used in the study of progressive fibrotic interstitial lung disease.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2170126-74-4
Sample solution is provided at 25 µL, 10mM.
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BMS-986278 is an orally active, high-affinity and potent small molecule LPA1 antagonist that is commonly used in the study of progressive fibrotic interstitial lung disease[1][2].
Cytotoxicity for BMS-986278( 0-100μM;24h,72h ) was not observed in human hepatocytes (IC50 >100 μM)[1]. 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[3].
BMS-986278 (30,100 and 300 mg/kg; 6 months) found centrilobular hepatocyte hypertrophy in the liver and gallbladder at 300 mg/kg/day and a dose-dependent increase in alkaline phosphatase (ALP) at all doses (≤ 2.3-fold), total bilirubin (TBILI) was dose-dependently increased (≤ 3.0-fold) only at the 100 mg/kg/day dose [2].BMS-986278(20, 50 and 100 mg/kg/day；1 month) produced a dose-dependent increase in plasma total bile acid (BA) levels in female monkeys [2].
References：
[1]. Gill MW, Murphy BJ, Cheng PTW, Sivaraman L, Davis M, Lehman-McKeeman L. Mechanism of hepatobiliary toxicity of the LPA1 antagonist BMS-986020 developed to treat idiopathic pulmonary fibrosis: Contrasts with BMS-986234 and BMS-986278. Toxicol Appl Pharmacol. 2022 Mar 1;438:115885.
[2]. Sivaraman L, Gill M, Nelson DM, Chadwick KD. Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA1) antagonists. Toxicol Appl Pharmacol. 2022 Mar 1;438:115846.
[3].Cheng PTW, Kaltenbach RF 3rd, Zhang H, et al.Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases. J Med Chem. 2021 Nov 11;64(21):15549-15581.
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