A potent and selective LPA1 receptor antagonist (IC50 = 17 nM); selective for LPA1 over the LPA2

AM966 – 1 mg

Brand:
Cayman
CAS:
1228690-19-4
Storage:
-20
UN-No:
Non-Hazardous - /

AM966 is an orally bioavailable, potent, and selective antagonist of the lysophosphatidic acid receptor 1 (LPA1) that has an IC50 value of 17 nM in a calcium assay using CHO cells transfected with the human LPA1 receptor.{36285} It is selective for LPA1 over the LPA2, LPA3, LPA4, and LPA5 receptors (IC50s = 1,700, 1,600, 7,700, and 8,600 nM for LPA2-5, respectively). In vitro, AM966 inhibits LPA-induced lung fibroblast cell chemotaxis (IC50 = 181 nM), increases barrier permeability, activates RhoA, and induces phosphorylation of myosin light chain and vascular endothelium cadherin (VE-cadherin).{36284,36283} At a dose of 30 mg/kg in mice, it reduces inflammation, tissue fibrosis, and vascular permeability following bleomycin-induced lung injury. AM966 also blocks amitriptyline-induced ERK1/2, CREB, and insulin growth factor-1 receptor (IGF-IR) phosphorylation in vitro.{36284}  

 

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Description

A potent and selective LPA1 receptor antagonist (IC50 = 17 nM); selective for LPA1 over the LPA2, LPA3, LPA4, and LPA5 receptors (IC50s = 1,700, 1,600, 7,700, and 8,600 nM for LPA2-5, respectively); inhibits LPA-induced lung fibroblast cell chemotaxis (IC50 = 181 nM); reduces inflammation, tissue fibrosis, and vascular permeability in mice at a dose of 30 mg/kg following bleomycin-induced lung injury; blocks amitriptyline-induced ERK1/2, CREB, and IGF-IR phosphorylation in vitro

Formal name: 4′-[4-[[[(1R)-1-(2-chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]-[1,1′-biphenyl]-4-acetic acid

Synonyms: 

Molecular weight: 490.9

CAS: 1228690-19-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation

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