| CAS NO: | 761423-87-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 404.45 |
|---|---|
| Formula | C21H21FOS |
| CAS No. | 761423-87-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 80 mg/mL (197.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 80 mg/mL (197.8 mM) | |
| Solubility (In vivo) | |
| Synonyms | ASP-1941; ASP1941; ASP 1941; Ipragliflozin |
| SMILES Code | O[C@H]1[C@H](C2=CC=C(F)C(CC3=CC4=CC=CC=C4S3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O |
| In Vitro | In vitro activity: Ipragliflozin inhibits mouse, rat, and human SGLT2 activity at low nanomolar concentrations. but it 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. Kinase Assay: Cell Assay: 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). |
|---|---|
| In Vivo | Ipragliflozin (Single oral doses of 0.01-10 mg/kg) 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%. 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. |
| Animal model | Male Sprague-Dawley rats |
| Formulation & Dosage | 0.01-10 mg/kg; Oral givage |
| References | Bioorg Med Chem. 2012 May 15;20(10):3263-79. |
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