产品说明

一般描述

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.
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.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Product competes with ATP.
Primary Target
P2X receptor
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

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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.

法律信息

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

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