AF-353|865305-30-2|-陌孚医药/Medlife

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AF-353

目录号: PL08673 纯度: ≥99%

CAS No. :865305-30-2

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中文名称	AF-353
中文别名	5-(5-碘-2-异丙基-4-甲氧基苯氧基)嘧啶-2,4-二胺;2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-
英文名称	AF-353
英文别名	2,4-Pyrimidinediamine, 5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-;5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine;AF 353;Ro-4;AF-353
Cas No.	865305-30-2
分子式	C₁₄H₁₇N₄O₂I
分子量	400.21
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	AF-353 (Ro-4) 是一种有效选择性、口服可利用的 P2X3/P2X2/3 受体拮抗剂, 抑制人和大鼠 P2X3 的 pIC₅₀ 值为 8.0，抑制人 P2X2/3 的 pIC₅₀ 值为 7.3。
生物活性	AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC 50 of 8.0 for both human and rat P2X3, and with a pIC 50 of 7.3 for human P2X2/3.
性状	Solid
IC50 & Target[1][2]	pIC50: 8.0 (human P2X3), 8.0 (rat P2X3), 7.3 (human P2X2/3)
体外研究(In Vitro)	AF-353 (Ro-4) 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 (Ro-4) also blocks human P2X2/3 channel function with marginally reduced potency with a p50 of 7.3. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	AF-353 (Ro-4) does not compromise oxygen levels or cardiac function. AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats. AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (249.87 mM; Need ultrasonic)配制储备液

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