SR 144528

Research use only, not for human use.

A highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.

A highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM; displays 700-fold lower affinity (Ki= 400 nM) for CB1 receptors, and no affinity for any of the more than 70 receptors, ion channels or enzymes (IC50>10 uM); antagonizes the inhibitory effects of CP 55,940 on forskolin-stimulated adenylyl cyclase activity with EC50 of 10 nM in cell-based assays, selectively blocks the MAPK activity induced by CP 55,940 with IC50 of 39 nM; displaces the ex vivo [3H]-CP 55,940 binding to mouse spleen membranes (ED50=0.35 mg/kg) with a long duration of action.

SR-144528;SR144528

GPCR/G Protein

Cannabinoid Receptor

Cannabinoid Receptor

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192703-06-3

476.05

C29H34ClN3O

>98% (HPLC)

DMSO : 50 mg/mL 105.03 mM

O=C(C1=NN(CC2=CC=C(C)C=C2)C(C3=CC=C(Cl)C(C)=C3)=C1)N[C@@H]4C(C)(C)[C@]5([H])CC[C@@]4(C)C5

5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years