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AF-353
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AF-353图片
CAS NO:865305-30-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
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。
Cas No.865305-30-2
别名Ro-4
Canonical SMILESCC(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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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.