Biochem/physiol Actions

Target IC₅₀: 140 nM suppressing the rate of GTPγS binding to Gsα-s-subunit

Primary TargetGsα-subunit-selective G-protein antagonist

Cell permeable: no

Reversible: no

Product does not compete with ATP.

General description

A potent G_sα-subunit-selective G-protein antagonist. Suppresses the rate of GTPγS binding to G_sα-s-subunit (IC₅₀ = 140 nM) but not to G_iα-1-subunit. Inhibits stimulation of adenylate cyclase activity in S49 cyc^- cells (which lack endogenous G_sα-subunit) by exogenously added G_sα-subunit. Also blocks the coupling of β-adrenergic receptors to G_s (EC₅₀ = 7.9 µM).

A potent G_sα-selective G-protein antagonist. Suppresses the rate of GTPγS binding to G_sα-s (IC₅₀ = 140 nM) but not in G_iα-1. Inhibits stimulation of adenylate cyclase activity in S49 cyc cells (which lack endogenous G_sα) by exogenously added G_sα-s. Also blocks the coupling of β-adrenergic receptors to G_s (EC₅₀ = 7.9 µM). Acts as a reversible competitive antagonist of the human P2X receptor, exhibiting much higher potency at human P2X(1) than at P2X(7) receptors (IC₅₀ = 50 nM vs 40 µM respectively).

Legal Information

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

Other Notes

Hulsmann, M., et al. 2003. Eur. J. Pharmacol.470, 1.Hohenegger, M., et al. 1998. Proc. Natl. Acad. Sci. USA 95, 346.

Packaging

10 mg in Glass bottle

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)