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活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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T407959-1ml |
1ml |
现货 ![]() |
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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)- |
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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 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 lines: Concentrations: Incubation Time: Powder Purity:≥99% |
IC50 | PDE5, IC50: 1.8 nM |
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分子类型 | 小分子 |
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Canonical SMILES | CN1CC(=O)N2C(CC3=C([NH]C4=C3C=CC=C4)C2C5=CC=C6OCOC6=C5)C1=O |
分子量 | 389.4 |
溶解性 | Solubility (25°C) In vitro DMSO: 4 mg/mL (10.82 mM); Water: Insoluble; Ethanol: Insoluble; |
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Concentration | 9-11(mmol/L) |
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Proton NMR spectrum | Conforms to Structure |