Home GPCR & G Protein SGLT inhibitor Ipragliflozin (ASP1941) For research use only.

Ipragliflozin (ASP1941)

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.

Ipragliflozin (ASP1941) Chemical Structure

Ipragliflozin (ASP1941) Chemical Structure

CAS: 761423-87-4

Purity & Quality Control

Batch: S863701 DMSO] 80 mg/mL] false] Ethanol] 80 mg/mL] false] Water] Insoluble] false Purity: 99.93%
99.93

Ipragliflozin (ASP1941) Related Products

Signaling Pathway

SGLT Signaling Pathways

SGLT Signaling Pathway

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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
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
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].
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 0.01-10 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02794792 Completed
Type 2 Diabetes Mellitus
Astellas Pharma Europe B.V.|Astellas Pharma Inc
 May 11 2016 Phase 3
NCT02529449 Completed
Type 1 Diabetes Mellitus
Astellas Pharma Inc
 September 1 2015 Phase 2
NCT01972880 Completed
Healthy|Plasma Concentration of ASP1941
Astellas Pharma Inc
 September 2013 Phase 1
NCT01611363 Completed
Type 2 Diabetes Mellitus
Astellas Pharma Europe B.V.|Astellas Pharma Inc
 October 27 2011 Phase 1
NCT01611415 Completed
Healthy Subjects|Pharmacokinetics of Ipragliflozin
Astellas Pharma Europe B.V.|Astellas Pharma Inc
 July 2011 Phase 1
NCT01611428 Completed
Bioavailability of Ipragliflozin|Healthy Subjects
Astellas Pharma Europe B.V.|Astellas Pharma Inc
 June 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 404.45 Formula

C21H21FOS
CAS No. 761423-87-4 SDF Download Ipragliflozin (ASP1941) SDF
Smiles C1=CC=C2C(=C1)C=C(S2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (197.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 80 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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