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Sildenafil Citrate.

(Synonyms: 西地那非柠檬酸盐; UK-92480 citrate)
目录号: PC12485 纯度: ≥98%
治疗勃起功能障碍和肺动脉高压(PAH)。Sildenafil citrate 是一种有效的磷酸二酯酶 5 (PDE5)抑制剂,IC50 为 5.22 nM。
CAS No. :171599-83-0
商品编号 规格 价格 会员价 是否有货 数量
PC12485-25mg 25mg ¥282.00 请登录
PC12485-50mg 50mg ¥404.00 请登录
PC12485-500mg 500mg ¥1415.00 请登录
PC12485-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥700.00 请登录
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中文名称
Sildenafil Citrate.
中文别名
枸橼酸西地那非;拘橼酸西地那非;1-[[3-(6,7-二氢-1-甲基-7-氧-3-丙基-1H-吡唑并-[4,3-d]嘧啶-5-基)-4-乙氧苯基]璜酰基]-4-甲基哌嗪柠檬酸盐;伟哥;西地那非柠檬酸盐;万艾可;西地那非(枸橼酸盐);艾万可西地那非;枸橼酸西地那非 EP标准品;枸橼酸西地那非 USP标准品;枸橼酸西地那非 标准品;枸橼酸西地那非(甾体);柠檬酸西地那非;西地那非;西地那非枸橼酸西地那非;西地那非柠檬酸盐标准品;西地那非杂质标准品对照品;1-[4-乙氧基-3-[5-(6,7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4,3-d]嘧啶)]苯磺酰]-4-甲基哌嗪枸橼酸盐;柠檬酸盐;5-[2-乙氧基-5-[(4-甲基哌嗪-1-基)磺酰基]苯基]-1-甲基-3-丙基-1H-吡唑并[4,3-d]嘧啶-7(6H)-酮柠檬酸盐;1-[[3-(4,7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4,3-d]嘧啶-5-基)-4-乙氧基苯基]磺酰基]-4-甲基哌嗪柠檬酸盐;柠檬酸喜地纳芬;西地那非(柠檬酸盐)
英文名称
Sildenafil Citrate
英文别名
Sildenafil citrate;1-[[3-(4,7-DIHYDRO-1-METHYL-7-OXO-3-PROPYL-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-ETHOXYPHENYL]SULFONYL]-4-METHYLPIPERAZINE, CITRATE;1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1h-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate;VIAGRA;piperazine,1-((3-(4,7-dihydro-1-methyl-7-oxo-3-propyl-1h-pyrazolo(4,3-d)pyrimi;piperazine,1-((3-(4,7-dihydro-1-methyl-7-oxo-3-propyl-1h-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methyl-,2-hydroxy-1,2,3-propanetricarboxylate(1:1);uk92480-10;SILDANAFIL CITRATE (BULK);SildenafilBaseC28H38N6O11S;SILDENAFIL CITRATE(RG);5(2-ETHOXY-5(4-METHYLPIPERAZINE)SULPHONYLPHENYL)-1;Sildenafil;Sildenafil citrate (UK-92480 citrate, Edegra®,Viagra®, Revatio®,Apodefil®,Kamagra®, Silagra®,Penegra®, Zenegra® );UK-92480 citrate;Viagra, Sildenafil citrate;steroids;5-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[4,3-d]pyrimidin-7-one,2-hydroxypropane-1,2,3-tricarboxylic acid;Sildenafil citrate salt;Viagra,Revatio;1-[[3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate salt;5-[2-Ethoxy-5-(4-methylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[5,4-e]pyrimidin-7-one citrate salt;Revatio;UK-92,480;5-[2-Ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one Citrate;[ "" ];Viagra citrate;Revatio citrate;ldenafil Citrate;Sildenafili citras;Methylpiperazine citrate;sidenafil;Sildenafil (citrate);Caverta;sildenafilcitrate;Sildenafil citrate [USAN];BW9B0ZE037;UK 92480;DSSTox_RID_81321;DSSTox_CID_26076;DSSTox_GSID_46076;1-((3-(6,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methylpiperazine citrate (1:1);5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimi;5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one 2-hydroxypropane-1,2,3-tricarboxylate;5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3
Cas No.
171599-83-0
分子式
C28H38N6O11S
分子量
666.70
包装储存

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

详情描述

治疗勃起功能障碍和肺动脉高压(PAH)。Sildenafil citrate 是一种有效的磷酸二酯酶 5 (PDE5)抑制剂,IC50 为 5.22 nM。

生物活性

Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

性状

Solid

IC50 & Target[1][2]

PDE5

 

体外研究(In Vitro)

Pretreatment with 1 μM Sildenafil citrate potentiates the phosphorylation of ERK1/ERK2, an increase in the percentage of cells in S phase and cell proliferation, compared with serotonin stimulation alone (P<0.05). Pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation leads to dramatic increase in OD value to 0.33, significantly different compared with serotonin stimulation alone (P<0.05). 1 μM Sildenafil obviously enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In the dog model of erection, Sildenafil citrate significantly increases ICP and ICP/BP but shows no significant effect on BP compared with vehicle. Sildenafil treatment significantly decreases the number of TL-cells at 10 but not 0.5 mg/kg. At this time point, cells positive for the M1-like marker COX-2 are found in the ischemic core in PBS-treated animals, whereas they are mostly observed in the penumbra in 10 mg/kg (but not 0.5 mg/kg) Sildenafil-treated animals. In contrast, 8 days after pMCAo the number of microglia/macrophages stained by Iba-1 are significantly reduced by Sildenafil treatment (0.5 and/or 10 mg/kg dose). Sildenafil citrate has been reported to decrease flap necrosis in preclinical animal models by increasing the secretion of growth factors (FGF and VEGF), and histologically is shown to be effective in rat cavernous nerve architecture.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 50 mg/mL (75.00 mM; Need ultrasonic)

H2O : 2 mg/mL (3.00 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4999 mL 7.4996 mL 14.9992 mL
5 mM 0.3000 mL 1.4999 mL 2.9998 mL
10 mM 0.1500 mL 0.7500 mL 1.4999 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (7.50 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (7.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (7.50 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (7.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (7.50 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (7.50 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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