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AF-353

目录号 : GC19022

AF-353 (Ro-4) 是一种有效的、选择性的和口服生物可利用的 P2X3/P2X2/3 受体拮抗剂,对人和大鼠 P2X3 的 pIC50 为 8.0,对人 P2X2/3 的 pIC50 为 7.3。

规格 价格 库存 购买数量
5mg
¥792.00
现货
10mg
¥1,395.00
现货
50mg
¥3,915.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2]

References:
[1]. Gever JR, et al. AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-1398.
[2]. Munoz A, et al. Modulation of bladder afferent signals in normal and spinal cord-injured rats by purinergic P2X3 and P2X2/3receptors. BJU Int. 2012 Oct;110(8 Pt B):E409-414.

Chemical Properties

Cas No. 865305-30-2 SDF
别名 Ro-4
化学名 N/A
Canonical SMILES CC(C)C1=C(OC2=CN=C(N)N=C2N)C=C(I)C(OC)=C1
分子式 C14H17IN4O2 分子量 400.21
溶解度 DMSO : ≥ 32 mg/mL (79.96 mM) 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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