480418

NF279

A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC₅₀/KB ~ 1 µM in smooth muscle).

• Synonyme(s) : NF279, 8,8ʹ-(Carbonylbis(imino-4,1-phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis-1,3,5-naphthalenetrisulfonic Acid, Na
• Formule empirique (notation de Hill): C₄₉H₃₀N₆O₂₃S₆ · 6Na
• Numéro CAS: 202983-32-2
• Poids moléculaire : 1401.12
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥99% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated; protect from light
• Couleur: white
• Solubilité: DMSO: 14 mg/mL; water: 35 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C49H36N6O23S6.6Na/c56-45(50-29-9-1-27(2-10-29)47(58)54-37-17-19-39(81(67,68)69)35-21-33(79(61,62)63)23-41(43(35)37)83(73,74)75)25-5-13-31(14-6-25)52-49(60)53-32-15-7-26(8-16-32)46(57)51-30-11-3-28(4-12-30)48(59)55-38-18-20-40(82(70,71)72)36-22-34(80(64,65)66)24-42(44(36)38)84(76,77)78;;;;;;/h1-24H,(H,50,56)(H,51,57)(H,54,58)(H,55,59)(H2,52,53,60)(H,61,62,63)(H,64,65,66)(H,67,68,69)(H,70,71,72)(H,73,74,75)(H,76,77,78);;;;;;/q;6*+1/p-6
• Clé InChI: RJMCMLNRWDKUDB-UHFFFAOYSA-H

Description

Description générale

A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC₅₀/K_B ~ 1 µM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no effect on α_1A adrenoceptors, adenosine A₁ and A_2B receptors, histamine H₁, muscarinic M₃ and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X₁ >P2X₂ >P2X₃ >P2X₄ (IC₅₀ = 19 nM, 770 nM, 1.62 µM and >300 µM, respectively) in Xenopus oocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X₁ > human P2X₁ > > rat P2X₂ > rat P2X₃ ~ human P2X₇ > > human P2X₄. Not degraded by ecto-nucleotidases.

A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC₅₀/K_B ~1 µM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no discernible effects on α_1A adrenoceptors, adenosine A₁ and A_2B receptors, histamine H₁, muscarinic M₃ and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X₁ >P2X₂ >P2X₃ >P2X₄ (IC₅₀ = 19 nM, 770 nM, 1.62 µM and >300 µM, respectively) in Xenopus oocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X₁ > human P2X₁ » rat P2X₂ > rat P2X₃ ~human P2X₇ » human P2X₄. Not degraded by ecto-nucleotidases.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
P2X receptor

Product competes with ATP.

Reversible: yes

Target IC₅₀: ~ 1 µM as antagonist of P2X receptor in smooth muscle; 19 nM, 770 nM, 1.62 µM and <300 µM, against P2X1, P2X2, P2X3, P2X4, respectively, in Xenopus oocytes pre-incubated with ATP

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Autres remarques

Klapperstück, M., et al. 2000. Eur. J. Pharmacol.387, 245.
Rettinger, J., et al. 2000. Neuropharmacol.39, 2044.
Lambrecht, G., et al. 1999. Prog. Brain Res.120,107.
Damer, S., et al. 1998. Eur. J. Pharmacol.350, R5.

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 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable