480420

NF449

A potent Gsα-subunit-selective G-protein antagonist.

• Synonyme(s) : NF449, 4,4ʹ,4ʹʹ,4ʹʹʹ-[Carbonyl- bis[imino-5,1,3-benzenetriyl bis-(carbonylimino)]]tetrakis-(benzene-1,3-disulfonic Acid, 8Na)
• Formule empirique (notation de Hill): C₄₁H₂₄N₆O₂₉S₈ · 8Na
• Numéro CAS: 627034-85-9
• Poids moléculaire : 1505.09
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: white
• Solubilité: distilled water: 100 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C41H32N6O29S8.8Na/c48-37(44-29-5-1-25(77(53,54)55)15-33(29)81(65,66)67)19-9-20(38(49)45-30-6-2-26(78(56,57)58)16-34(30)82(68,69)70)12-23(11-19)42-41(52)43-24-13-21(39(50)46-31-7-3-27(79(59,60)61)17-35(31)83(71,72)73)10-22(14-24)40(51)47-32-8-4-28(80(62,63)64)18-36(32)84(74,75)76;;;;;;;;/h1-18H,(H,44,48)(H,45,49)(H,46,50)(H,47,51)(H2,42,43,52)(H,53,54,55)(H,56,57,58)(H,59,60,61)(H,62,63,64)(H,65,66,67)(H,68,69,70)(H,71,72,73)(H,74,75,76);;;;;;;;/q;8*+1/p-8
• Clé InChI: KCBZSNWCUJBMHF-UHFFFAOYSA-F

Description

Description générale

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).

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).

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
Gsα-subunit-selective G-protein antagonist

Product does not compete with ATP.

Reversible: no

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

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable