| Bioactivity | 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[1]. | ||||||||||||
| Target | Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1) | ||||||||||||
| Invitro | 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[1].BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a Kb of 5.8 nM[1]. | ||||||||||||
| 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[1].BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats[1].Pharmacokinetics of BMS-986278 in preclinical species[1] | ||||||||||||
| Name | BMS-986278 | ||||||||||||
| CAS | 2170126-74-4 | ||||||||||||
| Formula | C22H31N5O5 | ||||||||||||
| Molar Mass | 445.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Cheng PTW, 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. |
BMS-986278
CAS: 2170126-74-4 F: C22H31N5O5 W: 445.51
BMS-986278 is a potent and orally active lysophosphatidic acid receptor 1 (LPA1) antagonist, with Kbs of 6.9 nM and 4.0
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