枸橼酸西地那非, 磷酸二酯酶 5A 抑制剂

PDE5 选择性抑制剂

2篇引用文献

10mM in DMSO

CAS编号: 171599-83-0(DMSO)
分子式: C₂₂H₃₀N₆O₄S·C₆H₈O₇
分子量: 666.7

有货

库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
S408547-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	1-[[3-(6,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine, 2-hydroxy-1,2,3-propanetricarboxylate
规格或纯度	10mM in DMSO
英文名称	Sildenafil Citrate
生化机理	枸橼酸西地那非是环磷酸鸟苷（cGMP）特异性 5 型磷酸二酯酶（PDE5）的选择性抑制剂，是一种耐受性良好且高效的勃起功能障碍治疗药物。
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	Information Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction. In vitro Sildenafil citrate is a potent PDE type 5 reversible and selective inhibitor that blocks cGMP hydrolysis effectively (Ki ∼3 nM). Sildenafil exhibited high affinity for PDE type 5 and type 6 with inhibition constants (Ki) of ∼3.5 and 33 nM, respectively.\xa0Sildenafil enhances sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths, suggesting that sildenafil augments the activity of NO-mediated relaxation. Sildenafil citrate increases intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside and in rabbit corpus cavernosum in vitro. Sildenafil is metabolized in the liver by cytochrome P450 and is converted into an active metabolite with characteristics similar to the parent compound. ^[1] In vivo Sildenafil citrate enhances erectile function following pelvic nerve stimulation in anesthetized dogs as measured by increased intracavernosal pressure. Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits. Sildenafil improves erectile function in a time- and dose-dependent fashion with maximization of erectile function recovery occurring with daily 20 mg/kg at the 28-day time point in Sprague-Dawley rats. Sildenafil use results in smooth muscle-collagen ratio protection and CD31 and eNOS expression preservation in Sprague-Dawley rats. Sildenafil reduces apoptotic indices significantly compared with control, and increases phosphorylation of akt and eNOS in Sprague-Dawley rats. Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥99%

产品属性

IC50	PDE5, IC50: 3.5 nM

关联靶点（人）

PDE5A Tclin cGMP 特异性 3',5'-环磷酸二酯酶(cGMP-specific 3',5'-cyclic phosphodiesterase) (3 活性数据)

点击查看靶蛋白信息： PDE5A

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	CCCC1=N[N](C)C2=C1N=C(NC2=O)C3=CC(=CC=C3OCC)[S](=O)(=O)N4CCN(C)CC4.OC(=O)CC(O)(CC(O)=O)C(O)=O
分子量	666.7

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 74 mg/mL (200.29 mM); Ethanol: 6 mg/mL warmed with 50ºC Water: bath (16.23 mM); Water: Insoluble;

安全和危险性（GHS）

SDS英文版

技术规格说明书

Concentration(Compounding value)	9.0-11.0（mmol/L）
Record the entire process by video	Conform

技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

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此产品的引用文献

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1. Ma Yufeng, Zhang Fengsen, Zhong Yijing, Huang Yongchun, Yixizhuoma , Jia Qiangqiang, Zhang Shoude. (2023) A label-free LC/MS-based enzymatic activity assay for the detection of PDE5A inhibitors. Frontiers in Chemistry, 11 [PMID:36860644] [10.3389/fchem.2023.1097027]
2. Shihua Yu, Zhigang Liu, Weixian Wang, Li Jin, Weiqing Xu, Yuqing Wu. (2018) Disperse magnetic solid phase microextraction and surface enhanced Raman scattering (Dis-MSPME-SERS) for the rapid detection of trace illegally chemicals. TALANTA, 178 (498). [PMID:29136854] [10.1016/j.talanta.2017.09.054]

参考文献

1. Ma Yufeng, Zhang Fengsen, Zhong Yijing, Huang Yongchun, Yixizhuoma , Jia Qiangqiang, Zhang Shoude. (2023) A label-free LC/MS-based enzymatic activity assay for the detection of PDE5A inhibitors. Frontiers in Chemistry, 11 [PMID:36860644] [10.3389/fchem.2023.1097027]
2. Shihua Yu, Zhigang Liu, Weixian Wang, Li Jin, Weiqing Xu, Yuqing Wu. (2018) Disperse magnetic solid phase microextraction and surface enhanced Raman scattering (Dis-MSPME-SERS) for the rapid detection of trace illegally chemicals. TALANTA, 178 (498). [PMID:29136854] [10.1016/j.talanta.2017.09.054]