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Home - Products - GPCR/G Protein - LPA Receptor - BMS-986278

BMS-986278

CAS No. 2170126-74-4

BMS-986278( —— )

Catalog No. M35137 CAS No. 2170126-74-4

BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BMS-986278
  • Note
    Research use only, not for human use.
  • Brief Description
    BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.
  • Description
    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.
  • In Vitro
    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.BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a Kb of 5.8 nM.
  • 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.BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats.Animal Model:Male Sprague-Dawley rats (10 weeks) were administered Bleomycin 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.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    LPA Receptor
  • Recptor
    LPA Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2170126-74-4
  • Formula Weight
    445.51
  • Molecular Formula
    C22H31N5O5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (224.46 mM; Ultrasonic )
  • SMILES
    CCCN(C)C(=O)OCc1c(nnn1C)-c1ccc(O[C@H]2CCC[C@@H](C2)C(O)=O)c(C)n1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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. ?
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