化合物Sildenafil Mesylate T6983

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

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途