A suramin analog that acts as a selective and direct G-protein antagonist for α-subunits of the Go/Gi group (EC50 ~ 300 nM). Suppresses GTPγS binding to recombinant G-protein α-subunits. Acts by inhibiting the formation of the agonist-specific ternary complex (agonist/receptor/G-protein). NF023 does not interfere with the interaction between α-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).
生物化学的/生理学的作用
Cell permeable: no
Primary Target α-subunits of the Go/Gi group of G-protein
Product does not compete with ATP.
Reversible: 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
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
再構成
Following reconstitution, aliquot and freeze (-20°C). Avoid freeze/thaw cycles of solutions.
その他情報
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.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany