化合物Sildenafil Mesylate T6983
面议
- TargetMol
- 生产商
- 进口
- 美国
- 现货
- 全国
- 4
- 1
Product IntroductionBioactivity英文名: Sildenafil Mesylate描述: Sildenafil Mesylate 是 Sildenafil 的甲磺酸盐形式，Sildenafil 是磷酸二酯酶 5 的
AI问答
配套的仪器设备？
可以搭配的相关耗材试剂？
耗材描述
Product Introduction
Bioactivity
英文名: Sildenafil Mesylate
描述: Sildenafil Mesylate 是 Sildenafil 的甲磺酸盐形式，Sildenafil 是磷酸二酯酶 5 的抑制剂。
体外活性: Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. [1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). [2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. [3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs <1 mg/L. [4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. [5]
体内活性: Chronic sildenafil treatment increases the detumescence phase in young and aged rats (p<0.05), although aged rats show a greater increase than young rats. Baseline cavernous PDE5 expression and activity are greater in aged vs young rats (p<0.05). After chronic sildenafil treatment cavernous PDE5 expression is increased in young (p<0.05) but not in aged rats. Chronic and acute sildenafil treatment similarly inhibits PDE5 activity in the penis of young and aged rats (p<0.05), coincident with its free plasma concentrations equivalent to clinically therapeutic ranges[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : 4 mg/mL0
H2O : 92 mg/mL
DMSO : 5.71 mg/mL (10 mM)
关键字: Sildenafil Mesylate
相关产品: Crisaborole | Enpp/Carbonic anhydrase-IN-1 | Ginkgolide J | Diphylline | TyK2-IN-2 | Lotamilast | ATX inhibitor 5 | Ro 20-1724 | Carbazeran | Autotaxin-IN-4
Bioactivity
英文名: Sildenafil Mesylate
描述: Sildenafil Mesylate 是 Sildenafil 的甲磺酸盐形式，Sildenafil 是磷酸二酯酶 5 的抑制剂。
体外活性: Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. [1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). [2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. [3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs <1 mg/L. [4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. [5]
体内活性: Chronic sildenafil treatment increases the detumescence phase in young and aged rats (p<0.05), although aged rats show a greater increase than young rats. Baseline cavernous PDE5 expression and activity are greater in aged vs young rats (p<0.05). After chronic sildenafil treatment cavernous PDE5 expression is increased in young (p<0.05) but not in aged rats. Chronic and acute sildenafil treatment similarly inhibits PDE5 activity in the penis of young and aged rats (p<0.05), coincident with its free plasma concentrations equivalent to clinically therapeutic ranges[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : 4 mg/mL0
H2O : 92 mg/mL
DMSO : 5.71 mg/mL (10 mM)
关键字: Sildenafil Mesylate
相关产品: Crisaborole | Enpp/Carbonic anhydrase-IN-1 | Ginkgolide J | Diphylline | TyK2-IN-2 | Lotamilast | ATX inhibitor 5 | Ro 20-1724 | Carbazeran | Autotaxin-IN-4
猜你喜欢
感兴趣产品