Sildenafil mesylate
(Synonyms:甲磺酸西地那非;3,3,20,20-双(亚乙二氧基)-5α,17α-二羟基-11β-[4-(N,N-二甲基氨基)-苯基]-19-去甲孕甾-9(11)-烯;水溶西地那非)
目录号 : KG10669
CAS No. : 1308285-21-3
纯度 : 98%
IC50: 3.5 nM
Sildenafil mesylate is an inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
PDE5 is the predominant phosphodiesterase in the corpus cavernosum. The catalytic site of PDE5 degrades cGMP, and PDE5 inhibitors can potentiate endogenous increases in cGMP.
In vitro: Sildenafil mesylate had been identified as a potent PDE5 reversible and selective inhibitor. Sildenafil enhanced sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths. Sildenafil also increased intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside .
In vivo: In anesthetized dogs, sildenafil could enhance the erectile function following pelvic nerve stimulation as measured by increased intracavernosal pressure .
Clinical trial: Ten previous randomised controlled trials had been conducted. Dose optimisation resulted in >60% of attempts at sexual intercourse, which was successful in 49% of men. Sildenafil treatment related adverse events occurred in 30% of men compared with 11% on placebo. Dose optimisation of sildenafil showed efficacy equivalent to the highest fixed doses, and adverse events equivalent to the lowest fixed doses .
Other Forms of Rapamycin:
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分子式 |
C23H34N6O7S2
|
分子量 |
570.68
|
CAS号 |
1308285-21-3
|
中文名称 |
甲磺酸西地那非
|
储存方式 |
Store at -20°C
|