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MRI-1891

Chemical Structure : MRI-1891

CAS No.: 2712480-46-9

MRI-1891 (Monlunabant, (S)-MRI-1891, MRI 1891, INV-202)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 591.01
Formula C26H22ClF3N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
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

References

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.

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