GAQ G PROTEIN INHIBITOR; BIM-46187

Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

General description

A cell-permeable tetrahydroimidazo[1,2a]pyrazine dimer that directly binds to GA subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish GA_q signaling in HEK294 and CHO cells via trapping GA_q in the empty pocket conformation by permitting GDP exit but interdicting GTP entry. In addition, elicits a dose-dependent analgesic effect in carrageenan-induced hyperalgesia (0.1-1 mg/kg, i.v.) and in a chronic constriction injury mouse model (0.3-3 mg/kg, i.v.), with synergistic effect when co-administered with morphine.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A cell-permeable tetrahydroimidazo[1,2a]pyrazine dimer that directly binds to GA subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish GA_q signaling in HEK294 and CHO cells via trapping GA_q in the empty pocket conformation by permitting GDP exit but interdicting GTP entry. In addition, elicits a dose-dependent analgesic effect in carrageenan-induced hyperalgesia (0.1-1 mg/kg, i.v.) and in a chronic constriction injury mouse model (0.3-3 mg/kg, i.v.), with synergistic effect when co-administered with morphine.r>r>Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Schmitz, A. et al. 1999. Chem. & Biol.21, 890.r>Ayoub, M. A., et al. 2009. J. Biol. Chem.284, 29136.r> Favre-Guilmard, C., et al. 2008. Eur. J. Pharm.594, 70.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Physical form

Supplied as a HCl salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)