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).

• Sinonimo/i: NF023, 8,8ʹ-[Carbonylbis(imino-3,1-phenylene)]bis-(1,3,5-naphthalenetrisulfonic Acid), 6Na, P2X Antagonist I, Purinergic Receptor P2X Antagonist I
• Formula empirica (notazione di Hill): C₃₅H₂₀N₄O₂₁S₆ · 6Na
• Peso molecolare: 1162.88
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic)
• Colore: white to off-white
• Solubilità: water: soluble
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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).

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable