阿伐那非, 磷酸二酯酶 5A 抑制剂

PDE5 选择性抑制剂
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
A408935-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 5-Pyrimidinecarboxamide, 4-[[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Avanafil
生化机理 阿伐那非是一种高选择性 PDE5 抑制剂,其 IC50 值为 5.2 nM,比其他 PDEs 的选择性高出 121 倍。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 磷酸二酯酶 5A 抑制剂
产品介绍

Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

Information

Avanafil is a highly selectivePDE5inhibitor withIC50of 5.2 nM, >121-fold selectivity over other PDEs.
In vitro


In vivo

Avanafil (i.v.) potentiates penile tumescence with ED200% of 37.5 μg/kg in dogs. Furthermore, intraduodenal treatment of Avanafil potentiates pelvic nerve stimulation induced changes in intracavernous pressure and duration. The cavernous injection of avanafil (1 μM) in T2DM rats results in partial improvement in erectile responses.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

IC50 PDE5, IC50: 1 nM
ALogP 2.165
hba_count 6
HBD Count 3
Rotatable Bond 9

关联靶点(人)

PDE5A Tclin cGMP 特异性 3',5'-环磷酸二酯酶(cGMP-specific 3',5'-cyclic phosphodiesterase) (25 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES COC1=C(Cl)C=C(CNC2=C(C=NC(=N2)N3CCCC3CO)C(=O)NCC4=NC=CC=N4)C=C1
分子量 483.95
Reaxy-Rn 38205117
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=38205117&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 74 mg/mL (200.31 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility 97
DMSO(mM) Max Solubility 200.43
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 38205117
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=38205117&ln=

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Appearance(A408935) Colorless Transparent Liquid
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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