Biochem/physiol Actions

Cell permeable: no

Target IC₅₀: 240 nM for P2X1; 8.5 µM for P2X3 receptor in rat muscle; 4.8 pM in the inhibition of excitatory junction potentials; EC50 ~ 300 nM as G-protein antagonist for α-subunits of the Go/Gi group

Reversible: no

Primary Targetα-subunits of the Go/Gi group of G-protein

Product does not compete with ATP.

General description

A suramin analog that acts as a selective G-protein antagonist for A-subunits of the G_o/G_i group (EC₅₀ ~300 nM). Suppresses GTPγS binding to recombinant G-protein A-subunits. Acts by inhibiting the formation of the agonist-specific ternary complex (agonist/receptor/G-protein). NF023 does not interfere with the interaction between A-subunits βγ-dimer but competes with the effector binding site. Also a P2X receptor antagonist (IC₅₀=0.24 µM for P2X1; 8.5 µM for P2X3 receptor in rat muscle).

A suramin analog that acts as a selective and direct G-protein antagonist for A-subunits of the G_o/G_i group (EC₅₀ ~ 300 nM). Suppresses GTPγS binding to recombinant G-protein A-subunits. Acts by inhibiting the formation of the agonist-specific ternary complex (agonist/receptor/G-protein). NF023 does not interfere with the interaction between A-subunits and βγ-dimer but competes with the effector binding site. Also a P2X receptor antagonist (IC₅₀ = 240 nM for P2X1; 8.5 µM for P2X3 receptor in rat muscle). Causes a concentration dependent inhibition of excitatory junction potentials (IC₅₀ = 4.8 pM).

Legal Information

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

Other Notes

Snedden, P., et al. 2000. Br. J. Pharmacol.129, 1089.Soto, F., et al. 1999. Neuropharmacology38, 141.Beindle, W., et al. 1996. Mol. Pharmacol.50, 415.Freissmuth, M., et al. 1996. Mol. Pharmacol.49, 602.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Avoid freeze/thaw cycles of solutions.

Warning

Toxicity: Standard Handling (A)