Sildenafil

製品コードS4684 バッチS468401

印刷

化学情報

 Chemical Structure Synonyms Revatio, UK-92480, Viagra Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C22H30N6O4S

分子量 474.58 CAS No. 139755-83-2
Solubility (25°C)* 体外 Water 14 mg/mL (29.49 mM)
DMSO Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.000mg/ml (2.11mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.000mg/ml (2.11mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Sildenafil(Revatio、UK-92480、Viagra)は、ホスホジエステラーゼ5阻害剤であり、IC50は5.22 nMです。
in vitro Sildenafil improves insulin signalling and NO production in endothelial cells, probably by reducing oxidative stress induced by hyperglycemia and by increasing intracellular Ca2+ levels.
in vivo Acute administration of the PDE-5 inhibitor sildenafil in a single clinically relevant dose does not modulate the in vivo function of the hypertrophic failing right heart of the rat measured by echocardiography and invasive hemodynamics.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HUVEC and HAEC
濃度 1 μM
反応時間 5 or 72 h
実験の流れ

HUVEC and HAEC from passages 3 to 6 are cultured for 72 hours in presence of 5.5 mmol/L glucose, 30 mmol/L glucose (high glucose; HG), 10 mmol/L Gluc-N with or without 1 µM of sildenafil (5 or 72 h) and/or 10−7 M insulin.

動物実験 動物モデル Wistar rats
投薬量 1 mg/kg
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/24618544/
  • https://pubmed.ncbi.nlm.nih.gov/21297971/

カスタマーフィードバック

Data from [Data independently produced by , , EXPERIMENTAL AND THERAPEUTIC MEDICINE, 2017, 13:2645-2650]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

miR-30d Attenuates Pulmonary Arterial Hypertension via Targeting MTDH and PDE5A and Modulates the Beneficial Effect of Sildenafil [ Adv Sci (Weinh), 2024, 11(40):e2407712] PubMed: 39206778
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Monitoring recovery after CNS demyelination, a novel tool to de-risk pro-remyelinating strategies [ Brain, 2023, 146(6):2453-2463] PubMed: 36995973
Additive protective effects of sacubitril/valsartan and bosentan on vascular remodelling in experimental pulmonary hypertension [ Cardiovasc Res, 2021, 117(5):1391-1401] PubMed: 32653925
(Curcumin+sildenafil) enhances the efficacy of 5FU and anti-PD1 therapies in vivo. [ J Cell Physiol, 2020, 10.1002/jcp.29580] PubMed: 31985048
Kyoto probe-1 reveals phenotypic differences between mouse ES cells and iTS-P cells [ Sci Rep, 2020, 10(1):18084] PubMed: 33093580
Skeletal restoration by phosphodiesterase 5 inhibitors in osteopenic mice: Evidence of osteoanabolic and osteoangiogenic effects of the drugs. [ Bone, 2020, 10.1016/j.bone.2020.115305] PubMed: 32126313
The role of PDE5a in oocyte maturation of zebrafish. [ Gen Comp Endocrinol, 2020, 286:113303] PubMed: 31654676
Neratinib augments the lethality of [regorafenib + sildenafil] [Booth L J Cell Physiol, 2019, 234(4):4874-4887] PubMed: 30203445
Palbociclib augments Neratinib killing of tumor cells that is further enhanced by HDAC inhibition [Booth L Cancer Biol Ther, 2018, 10.1080/15384047.2018.1507665] PubMed: 30183517

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。