| Company Name: |
ShangHai Caerulum Pharma Discovery Co., Ltd. Gold
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| Tel: |
15000803246 18149758185 |
| Email: |
sales-cpd@caerulumpharma.com |
| Products Intro: |
Product Name:Admilparant; BMS-986278
CAS:2170126-74-4
Purity:99% Package:1g;10g;100g
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| Company Name: |
Suzhou Kangda Pharmaceutical Co., Ltd Gold
|
| Tel: |
18912614918 |
| Email: |
yaru.liu@kdbiopharma.com |
| Products Intro: |
Product Name:BMS-986278
CAS:2170126-74-4
Purity:97% Package:1;10;100;1000
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| | BMS-986278 Basic information |
| Product Name: | BMS-986278 | | Synonyms: | BMS-986278;(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;BMS-986278, 10 mM in DMSO;BMS-986278-01;Admilparant | | CAS: | 2170126-74-4 | | MF: | C22H31N5O5 | | MW: | 445.52 | | EINECS: | | | Product Categories: | | | Mol File: | 2170126-74-4.mol |  |
| | BMS-986278 Chemical Properties |
| 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 Usage And Synthesis |
| 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 |
| | BMS-986278 Preparation Products And Raw materials |
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