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
* <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 concentration-dependently inhibits mouse, rat, and human SGLT2 activity at nanomolar concentrations. Furthermore, ipragliflozin does not potently inhibit human SGLT4 and SGLT5 isoforms (IC50>1,000 nM). In addition, ipragliflozin 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). Ipragliflozin 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. Ipragliflozi is stable against mouse intestinal glucosidases[2].
in vivo Single oral doses (0.01-10 mg/kg) of ipragliflozin induces urinary glucose excretion in a dose-dependent manner in both normal and in KK-Ay mice, a type 2 diabetes model. Single administrations of ipragliflozin (0.1, 0.3 and 1 mg/kg) dose-dependently reduces 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 ipragliflozin has good bioavailability with a value of 71.7%[1]. Ipragliflozin shows good pharmacokinetic properties following oral dosing, and dose-dependently increased 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 ipragliflozin (3 mg/kg) to normal mice, plasma concentrations of ipragliflozin 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, ipragliflozin shows good oral bioavailability and exhibits high drug concentrations for long periods. The absolute bioavailabilities of ipragliflozin 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

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。

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