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).

• Sinonimo/i: NF279, 8,8ʹ-(Carbonylbis(imino-4,1-phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis-1,3,5-naphthalenetrisulfonic Acid, Na
• Formula empirica (notazione di Hill): C₄₉H₃₀N₆O₂₃S₆ · 6Na
• Numero CAS: 202983-32-2
• Peso molecolare: 1401.12
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥99% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated; protect from light
• Colore: white
• Solubilità: DMSO: 14 mg/mL; water: 35 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 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; RJMCMLNRWDKUDB-UHFFFAOYSA-H

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

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