Ipragliflozin (ASP1941)

製品コードS8637 バッチS863701

印刷

化学情報

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

C21H21FOS
分子量 404.45 CAS No. 761423-87-4
Solubility (25°C)* 体外 DMSO 80 mg/mL (197.79 mM)
Ethanol 80 mg/mL (197.79 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
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。

 4mg/ml (9.89mM) Taking the 1 mL working solution as an example, add 50 μL of 80 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。

 0.57mg/ml (1.41mM) Taking the 1 mL working solution as an example, add 50 μL of 11.4 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 Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1.
in vitro Ipragliflozin (ASP1941) concentration-dependently inhibits mouse, rat, and human SGLT2 activity at nanomolar concentrations. Furthermore, it does not potently inhibit human SGLT4 and SGLT5 isoforms (IC50>1,000 nM). In addition, this compound does not inhibit several glucose transporter (GLUT) isoforms, including GLUT1 and GLUT4, in mouse 3T3-L1, rat L6, human Caco-2, and HepG2 cells (IC50>1,000 nM). It does not interact with various receptors, ion channels, and transporters such as adrenergic (α1, α2, and β), muscarinic (M1, M2, and non-selective), angiotensin(AT1 and AT2), calcium channel (L-type and N-type), potassium channel (KATP and SKCa), sodium channel (site 2), cholecystokinin (CCKA and CCKB), dopamine (D1, D2, and transporter), endothelin (ETA and ETB), gamma-aminobutyric acid (GABAA and GABAB), glutamate (AMPA, kainate, and NMDA), serotonin (5-HT1, 5HT2B, and transporter), histamine (H1, H2, and H3), and neurokinin (NK1, NK2, and NK3), exhibiting IC50 values >3,000 nM. It is stable against mouse intestinal glucosidases[2].
in vivo Single oral doses (0.01-10 mg/kg) of ipragliflozin (ASP1941) induce urinary glucose excretion in a dose-dependent manner in both normal and KK-Ay mice, a type 2 diabetes model. Single administrations of this compound (0.1, 0.3 and 1 mg/kg) dose-dependently reduce blood glucose level in both KK-Ay mice and STZ rats. Administration of a single 0.3 mg/kg dose intravenously and a single 1 mg/kg dose orally to rats reveal that it has good bioavailability with a value of 71.7%[1]. It shows good pharmacokinetic properties following oral dosing, and dose-dependently increases urinary glucose excretion, which lasts for over 12 h in normal mice. Single administration of ipragliflozin results in dose-dependent and sustained antihyperglycemic effects in both diabetic models. It has a low risk of hypoglycemia. After oral administration of the compound (3 mg/kg) to normal mice, plasma concentrations reach a maximum at 1 h and then gradually decrease. Obvious plasma concentrations are detected even 8 h after administration. In the pharmacokinetic studies in mice, it shows good oral bioavailability and exhibits high drug concentrations for long periods. The absolute bioavailabilities are 71.7-90.7% and 74.5-75.3% in rats and monkeys, respectively [2].

プロトコル(参考用のみ)

動物実験 動物モデル Male Sprague-Dawley rats
投薬量 0.01-10 mg/kg
投与方法 oral

参考

  • https://pubmed.ncbi.nlm.nih.gov/22507206/
  • https://pubmed.ncbi.nlm.nih.gov/22139434/

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。