Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MRI-1891
CAS No.: 2712480-46-9
Catalog No.: PC-20170Not For Human Use, Lab Use Only.
MRI-1891 (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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $388 | In stock | |
| 10 mg | $578 | In stock | |
| 25 mg | $958 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
| M.Wt | 591.01 | |
| Formula | C26H22ClF3N6O3S | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
N-[[[[(4S)-3-(4-Chlorophenyl)-4,5-dihydro-4-phenyl-1H-pyrazol-1-yl][[[4-(trifluoromethyl)phenyl]sulfonyl]amino]methylene]amino]iminomethyl]acetamide |
|
1. Ziyi Liu , et al. ACS Pharmacol Transl Sci. 2021 Apr 8;4(3):1175-1187.
2. Ghosh A, et al. Eur J Pharmacol. 2023 Apr 5;944:175589.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
