Ipragliflozin (ASP1941)

For research use only.

Catalog No.S8637

Ipragliflozin (ASP1941) Chemical Structure

Molecular Weight(MW): 404.45

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.

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Biological Activity

Description 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.
Targets
mouse SGLT2 [2]
(cell-free)
rat SGLT2 [2]
(cell-free)
hSGLT2 [1]
(cell-free)
5.64 nM 6.73 nM 7.4 nM
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].

Protocol

Animal Research:

[1]

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  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 0.01-10 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (197.79 mM)
Ethanol 80 mg/mL (197.79 mM)
Water 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.

Chemical Information

Molecular Weight 404.45
Formula

C21H21FOS

CAS No. 761423-87-4
Storage powder
in solvent
Synonyms N/A
Smiles OCC1OC(C(O)C(O)C1O)C2=CC(=C(F)C=C2)CC3=CC4=C(S3)C=CC=C4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02794792 Completed Drug: Ipragliflozin L-proline|Drug: Metformin|Drug: Placebo Type 2 Diabetes Mellitus Astellas Pharma Europe B.V.|Astellas Pharma Inc May 11 2016 Phase 3
NCT02529449 Completed Drug: Placebo|Drug: ASP1941 Type 1 Diabetes Mellitus Astellas Pharma Inc September 1 2015 Phase 2
NCT01972880 Completed Drug: ASP1941 Healthy|Plasma Concentration of ASP1941 Astellas Pharma Inc September 2013 Phase 1
NCT01611363 Completed Drug: ASP1941|Drug: Placebo Type 2 Diabetes Mellitus Astellas Pharma Europe B.V.|Astellas Pharma Inc October 27 2011 Phase 1
NCT01611415 Completed Drug: Ipragliflozin|Drug: Furosemide Healthy Subjects|Pharmacokinetics of Ipragliflozin Astellas Pharma Europe B.V.|Astellas Pharma Inc July 2011 Phase 1
NCT01611428 Completed Drug: Ipragliflozin Bioavailability of Ipragliflozin|Healthy Subjects Astellas Pharma Europe B.V.|Astellas Pharma Inc June 2011 Phase 1

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SGLT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID