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体外研究 (In Vitro) |
当1 μM西地那非预处理代替单独的5-羟色胺刺激时,可以改善ERK1/ERK2的磷酸化,增加S期细胞的百分比,促进细胞增殖(P<0.05)。 1 μM枸橼酸西地那非预处理和5-羟色胺刺激后,OD值急剧增加至0.33,与单独5-羟色胺刺激有显着差异(P<0.05)。 1 μM 西地那非显着增加了血清素引起的 ERK1/ERK2 磷酸化 [2]。
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体内研究 (In Vivo) |
西地那非显着提高了犬勃起模型中的 ICP 和 ICP/BP,但与媒介物相比,它对血压没有明显影响 [1]。在 10 mg/kg 的剂量下,西地那非治疗显着减少了 TL+- 细胞的数量。 pMCAo 后八天,西地那非治疗(0.5 和/或 10 mg/kg 剂量)显着减少了 Iba-1 染色的小胶质细胞/巨噬细胞的数量 [3]。根据临床前动物模型,西地那非可以通过分泌更多的生长因子(FGF和VEGF)来减少皮瓣坏死。组织学也已证明它对大鼠海绵状神经结构有益[4]。
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动物实验 |
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参考文献 |
[1]. Wang Z, et al. The Selectivity and Potency of the New PDE5 Inhibitor TPN729MA. J Sex Med. 2013 Nov;10(11):2790-7.
[2]. Li BB, et al. Sildenafil potentiates the proliferative effect of porcine pulmonary artery smooth muscle cells induced by serotonin in vitro. Chin Med J (Engl). 2011 Sep;124(17):2733-40. [3]. Moretti R, et al. Sildenafil, a cyclic GMP phosphodiesterase inhibitor, induces microglial modulation after focal ischemia in the neonatal mouse brain. J Neuroinflammation. 2016 Apr 28;13(1):95. [4]. Korkmaz MF, et al. The Effect of Sildenafil on Recuperation from Sciatic Nerve Injury in Rats. Balkan Med J. 2016 Mar;33(2):204-11 |
分子式 |
C22H30N6O4S
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分子量 |
474.58
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CAS号 |
139755-83-2
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相关CAS号 |
Sildenafil citrate;171599-83-0;Sildenafil-d3;1126745-90-1;Sildenafil-d8;951385-68-5;Sildenafil Mesylate;1308285-21-3;Sildenafil-d3N-1;1126745-87-6
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SMILES |
CN1CCN(S(=O)(C2=CC=C(OCC)C(C(NC3=C4N(C)N=C3CCC)=NC4=O)=C2)=O)CC1
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InChi Key |
BNRNXUUZRGQAQC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H30N6O4S/c1-5-7-17-19-20(27(4)25-17)22(29)24-21(23-19)16-14-15(8-9-18(16)32-6-2)33(30,31)28-12-10-26(3)11-13-28/h8-9,14H,5-7,10-13H2,1-4H3,(H,23,24,29)
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化学名 |
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-
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别名 |
UK-92480; UK 92480-10; UK 92480; UK92480 citrate; UK-92,480-10. Trade names: Revatio.
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL Solubility in Formulation 4: ≥ 10 mg/mL (21.07 mM) (saturation unknown) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1071 mL | 10.5356 mL | 21.0713 mL | |
5 mM | 0.4214 mL | 2.1071 mL | 4.2143 mL | |
10 mM | 0.2107 mL | 1.0536 mL | 2.1071 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
Sildenafil enhances the lethality of [pemetrexed + sorafenib].Oncotarget. 2017 Feb 21; 8(8): 13464–13475. td> |
[Pemetrexed + sorafenib + sildenafil] treatment inactivates cyto-protective STAT3, STAT5 and AKT whilst reducing the expression of cyto-protective proteins MCL-1, BCL-XL and Thioredoxin.Oncotarget. 2017 Feb 21; 8(8): 13464–13475. td> |
Sildenafil-induced PKG signaling plays a greater role in enhancing [pemetrexed + sorafenib] toxicity than nitric oxide synthase signaling.Oncotarget. 2017 Feb 21; 8(8): 13464–13475. td> |