BMS-986278
- Product Name
- BMS-986278
- CAS No.
- 2170126-74-4
- Chemical Name
- BMS-986278
- Synonyms
- BMS-986278;Admilparant;BMS-986278-01;BMS-986278, 10 mM in DMSO;(1S,3S)-3-((2-Methyl-6-(1-methyl-5-(((methyl(propyl)carbamoyl)oxy)methyl)-1H-1,2,3-triazol-4-yl)pyridin-3-yl)oxy)cyclohexane-1-carboxylic acid;Cyclohexanecarboxylic acid, 3-[[2-methyl-6-[1-methyl-5-[[[(methylpropylamino)carbonyl]oxy]methyl]-1H-1,2,3-triazol-4-yl]-3-pyridinyl]oxy]-, (1S,3S)-
- CBNumber
- CB59922283
- Molecular Formula
- C22H31N5O5
- Formula Weight
- 445.52
- MOL File
- 2170126-74-4.mol
BMS-986278 Property
- 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|
BMS-986278 Chemical Properties,Usage,Production
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. |
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
BMS-986278 Preparation Products And Raw materials
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