西力士, 磷酸二酯酶 5A 抑制剂

PDE5 选择性抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
T407959-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 Pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6R,12aR)-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Tadalafil (IC351)
生化机理 他达拉非(IC351)是一种 PDE-5 抑制剂,在无细胞试验中的 IC50 值为 1.8 nM。他达拉非对 PDE5 的选择性至少是其他大多数 PDE 家族(PDE11 除外)的 9000 倍。它可以部分抑制 PDE11
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

adalafil是一种PDE-5抑制剂,IC50为1.8 nM。A phosphodiesterase 5 inhibitor

Information

Tadalafil (IC351) is aPDE-5inhibitor withIC50of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibitsPDE11
In vitro

Tadalafil binds to PDE5 with KD of 2.4 nM. cGMP stimulates the binding of [3H]Tadalafil. Tadalafil (1 mM) results increased CYP3A protein expression in human hepatocytes.

In vivo

Tadalafil (2 mg/kg) almost completely restores penile oxygenation and abolishes neurotomy induced increase and substantially rescues muscle/fiber ratio in penile sectionsin sham-operated rats. Tadalafil (2 mg/kg or 10 mg/kg) significantly improves neurological functional recovery and increases cerebral vascular density and the percentage of BrdU-positive endothelial cells around the ischemic boundary. Tadalafil selectively increases cGMP but not cAMP in brain of rats. Tadalafil decreases the number of apoptotic cells and increases the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

IC50 PDE5, IC50: 1.8 nM

关联靶点(人)

PDE11A Tchem 双 3',5'-环-AMP 和 -GMP 磷酸二酯酶 11A(Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A) (10 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)
PDE5A Tclin cGMP 特异性 3',5'-环磷酸二酯酶(cGMP-specific 3',5'-cyclic phosphodiesterase) (18 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)
PDE6C Tclin 锥体 cGMP 特异性 3',5'-环磷酸二酯酶亚基 α'(Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha') (1 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 CN1CC(=O)N2C(CC3=C([NH]C4=C3C=CC=C4)C2C5=CC=C6OCOC6=C5)C1=O
分子量 389.4

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 4 mg/mL (10.82 mM); Water: Insoluble; Ethanol: Insoluble;

安全和危险性(GHS)

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

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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