MRI-1891 (Monlunabant, INV-202) | CB1R antagonist | Probechem Biochemicals

Chemical Structure : MRI-1891

CAS No.: 2712480-46-9

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

货号: 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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5 mg	￥3880	In stock
10 mg	￥5780	In stock
25 mg	￥9580	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	591.01
分子式	C26H22ClF3N6O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.

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

生物&药学活性

物理化学性质&存储条件

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

生物&药学活性

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