| 产品介绍 |
MRI-1891 (Monlunabant, INV-202) is potent, selective, β-Arrestin-2-biased peripheral cannabinoid-1 receptor (CB1R) antagonist with Ki of 0.3 nM (hCB1R), >2000-fold CB1R/CB2R selectivity.
MRI-1891 displays high bias toward inhibiting CB1R-agonist-induced β-arrestin-2 (βArr2) recruitment (IC50=21 pM) versus inhibiting CB1R-agonist-induced G protein activation, as monitored by GTPγS binding (IC50=6 nM).
In C2C12 myoblasts, CB1R activation suppresses insulin-induced akt-2 phosphorylation, preventable by MRI-1891
MRI-1891 improves obesity-induced muscle insulin resistance in wild-type but not in βArr2-KO mice.
MRI-1891 augments glucose stimulated insulin secretion in isolated human pancreatic islets and mouse islets, shows comparable insulin secretion enhancing effect to exendin-4.
MRI-1891 treatment protects isolated human islet cells against cytokine-induced apoptosis, similar to exendin-4.
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