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Beschreibung

A cell-permeable tetrahydroimidazo[1,2a]pyrazine dimer that directly binds to G&alpha, subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish G&alpha,q signaling in HEK294 and CHO cells via trapping G&alpha,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 G&alpha, subunit and inhibits heterotrimeric G protein signaling. Shown to selectively abolish G&alpha,q signaling in HEK294 and CHO cells via trapping G&alpha,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.