Avanafil

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Avanafil

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。

CAS NO:

330784-47-9

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
50mg	电议

产品介绍

Avanafil (TA-1790) 是一种有效的选择性磷酸二酯酶 5 (PDE-5) 抑制剂，对 PDE- 的 IC50 值为 5.2 nM、630 nM、5700 nM、6200 nM、12000 nM、27000 nM、51000 nM 和 53000 nM。 5、PDE-6、PDE-4、PDE-10、PDE-8、PDE-7、PDE-2 和 PDE-1。

Cas No.	330784-47-9
别名	阿伐那非; TA1790
化学名	(S)-4-((3-chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide
Canonical SMILES	O=C(C1=CN=C(N2[C@H](CO)CCC2)N=C1NCC3=CC=C(OC)C(Cl)=C3)NCC4=NC=CC=N4
分子式	C₂₃H₂₆ClN₇O₃
分子量	483.95
溶解度	≥ 17.6 mg/mL in DMSO
储存条件	Store at -20℃
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
产品描述	Avanafil is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) with IC50 value of 5.2nM [1]. PDE5 is abundantly expressed in penile corpus cavernosum and regulates penile blood flow by regulating the cGMP concentration. PDE5 inhibitors are similar in structure to cGMP and competitively bind to PDE5, resulting in the inhibition of cGMP hydrolysis. Avanafil is a high selective inhibitor of PDE5 with Ki value of 4.3nM and is developed for the treatment of erectile dysfunction. It shows high selectivity against other PDE enzymes of the PDE family. In the intravenous study, the administration of avanafil at 300μg/kg can potentiate penile tumescence. The calculated ED200% of avanafil on tumescence is 37.5μg/kg and the plasma concentration is 59.6ng/ml. Additionally, avanafil potentiates penile tumescence at a dose range of 100 to 1,000μg/kg intraduodenally. And the ED200% is 151.7μg/kg [1, 2]. References: [1] Kotera J, Mochida H, Inoue H, Noto T, Fujishige K, Sasaki T, Kobayashi T, Kojima K, Yee S, Yamada Y, Kikkawa K, Omori K. Avanafil, a potent and highly selective phosphodiesterase-5 inhibitor for erectile dysfunction. J Urol. 2012 Aug;188(2):668-74. [2] Cui YS, Li N, Zong HT, Yan HL, Zhang Y. Avanafil for male erectile dysfunction: a systematic review and meta-analysis. Asian J Androl. 2014 May-Jun;16(3):472-7.