480415

NF023

A suramin analog that acts as a selective and direct G-protein antagonist for α-subunits of the Go/Gi group (EC₅₀ ~ 300 nM).

• Synonym(s): NF023, 8,8ʹ-[Carbonylbis(imino-3,1-phenylene)]bis-(1,3,5-naphthalenetrisulfonic Acid), 6Na, P2X Antagonist I, Purinergic Receptor P2X Antagonist I
• Empirical Formula (Hill Notation): C₃₅H₂₀N₄O₂₁S₆ · 6Na
• Molecular Weight: 1162.88
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• color: white to off-white
• solubility: water: soluble
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A suramin analog that acts as a selective G-protein antagonist for α-subunits of the G_o/G_i 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 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 α-subunits of the G_o/G_i 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).

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable