Tadalafil

製品コードS1512 バッチS151204

印刷

化学情報

Chemical Structure Synonyms IC351 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H19N3O4
分子量 389.4 CAS No. 171596-29-5
Solubility (25°C)* 体外 DMSO 88 mg/mL (225.98 mM)
Water 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
3.9mg/ml Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 78 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; 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. 
* <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 Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11
in vitro Tadalafil binds to PDE5 with KD of 2.4 nM. cGMP stimulates the binding of [3H]Tadalafil. [1] Tadalafil (1 mM) results increased CYP3A protein expression in human hepatocytes. [2]
in vivo Tadalafil (2 mg/kg) almost completely restores penile oxygenation and abolishes neurotomy induced increase and substantially rescues muscle/fiber ratio in penile sectionsin sham-operated rats. [3] Tadalafil (2 mg/kg or 10 mg/kg) significantly improves neurological functional recovery and increases cerebral vascular density and the percentage of BrdU-positive endothelial cells around the ischemic boundary. Tadalafil selectively increases cGMP but not cAMP in brain of rats. [4] Tadalafil decreases the number of apoptotic cells and increases the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice. [5]
特徴 Much more potent to PDE-5 than PDE-1 or PDE-6.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assays
Binding reaction mixture containing the enzyme is incubated on ice or in a 30 ℃ water bath for 45 min. Nitrocellulose membranes (0.45 μm) are placed under house vacuum and prewetted with 1 mL of ice-cold 10 mM potassium phosphate, pH 6.8, that contained 0.1% Triton X-100. Next, 200 μL of 25% Triton X-100 at room temperature in KPM is added to the reaction tube. The entire contents of the tube are applied to the prewetted filter. The reaction tube is then washed with 3 mL of cold 0.1% Triton X-100 in 10 mM potassium phosphate, pH 6.8, and the wash is also applied to the filter. Filter membranes are removed, dried, and transferred to 6 mL scintillation vials. Nonaqueous scintillant (5 mL) is added to the tubes, which are then placed in a scintillation counter.
動物実験 動物モデル Sham-operated rats
投薬量 2 mg/kg
投与方法 Orally

カスタマーフィードバック

Data from [Data independently produced by Cell Death Dis, 2014, 5, e1544]

Data from [Data independently produced by , , J Cell Physiol, 2015, 230(7): 1661-76]

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：

RGS2-mediated translational control mediates cancer cell dormancy and tumor relapse [ J Clin Invest, 2021, 131(1)136779] PubMed: 33393490
Tadalafil enhances the therapeutic efficacy of BET inhibitors in hepatocellular carcinoma through activating Hippo pathway [ Biochim Biophys Acta Mol Basis Dis, 2021, 1867(12):166267] PubMed: 34508829
Tadalafil impacts the mechanical properties of Plasmodium falciparum gametocyte-infected erythrocytes [ Mol Biochem Parasitol, 2021, 244:111392] PubMed: 34171456
Impaired Redox and Protein Homeostasis as Risk Factors and Therapeutic Targets in Toxin-Induced Biliary Atresia [ Gastroenterology, 2020, 159(3):1068-1084.e2] PubMed: 32505743
Critical Impact of Drug-Drug Interactions via Intestinal CYP3A in the Risk Assessment of Weak Perpetrators Using Physiologically Based Pharmacokinetic Models. [ Drug Metab Dispos, 2020, 48(4):288-296] PubMed: 31996361
The role of PDE5a in oocyte maturation of zebrafish. [ Gen Comp Endocrinol, 2020, 286:113303] PubMed: 31654676
RhoBTB1 protects against hypertension and arterial stiffness by restraining phosphodiesterase 5 activity. [ J Clin Invest, 2019, 129(6):2318-2332] PubMed: 30896450
Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression. [ Cancers (Basel), 2019, 11(11)] PubMed: 31698786
Activation of cGMP/PKG/p65 signaling associated with PDE5-Is downregulates CCL5 secretion by CD8 + T cells in benign prostatic hyperplasia [ Prostate, 2019, 79(8):909-919] PubMed: 30958912
Targeting the crosstalk between cytokine-induced killer cells and myeloid-derived suppressor cells in hepatocellular carcinoma [Yu SJ, et al. J Hepatol, 2018, 10.1016/j.jhep.2018.10.040] PubMed: 30414862

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。