| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [form ]
Solid | [color ]
White to light yellow | [InChIKey]
UEUNDURNLYLSNB-DPLXLLBNNA-N | [SMILES]
C(C1N(N=NC=1C1=CC=C(O[C@H]2CCC[C@H](C(=O)O)C2)C(C)=N1)C)OC(=O)N(C)CCC |&1:11,15,r| |
| Hazard Information | Back Directory | [Uses]
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]. | [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]
| plasma clearance ((mL/min)/kg) | Vss (L/kg) | oral bioavailability (%) | T1/2 (h) | plasma protein binding (% free) | | mouse | 37 | 5.5 | 70 | 2.5 | 31.4 | | rat | 15 | 3.5 | 100 | 4.5 | 12.6 | | monkey | 2.0 | 1.6 | 79 | 11 | 0.8 |
| Animal Model: | Male Sprague-Dawley rats (10 weeks) were administered Bleomycin[1] | | 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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| [References]
[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. DOI:10.1021/acs.jmedchem.1c01256 |
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Tel: |
020-13556033878 2965585218 13556033878 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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