AM966, CAS 1228690-19-4

Formulation: A crystalline solid

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

Purity: ≥98%

Formula Markup: C27H23ClN2O5

Formula Weight: 490,9

Shelf life (days): 1460

CAS Number: 1228690-19-4

Notes: 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}

• Artikelnummer: CAY22048-1
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 22048-1
• Green Labware: Nein
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK