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).

• Synonim(y): NF279, 8,8ʹ-(Carbonylbis(imino-4,1-phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis-1,3,5-naphthalenetrisulfonic Acid, Na
• Wzór empiryczny (zapis Hilla): C₄₉H₃₀N₆O₂₃S₆ · 6Na
• Numer CAS: 202983-32-2
• Masa cząsteczkowa: 1401.12
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥99% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated; protect from light
• kolor: white
• rozpuszczalność: DMSO: 14 mg/mL; water: 35 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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
• Klucz InChI: RJMCMLNRWDKUDB-UHFFFAOYSA-H

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable