Ipragliflozin (ASP1941)

Catalog No.S8637 Batch:S863701

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Technical Data

Formula

C21H21FOS
Molecular Weight 404.45 CAS No. 761423-87-4
Solubility (25°C)* In vitro DMSO 80 mg/mL (197.79 mM)
Ethanol 80 mg/mL (197.79 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
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

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 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

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (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 results in dose-dependent and sustained antihyperglycemic effects in both diabetic models. It has a low risk of hypoglycemia. After oral administration (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].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    0.01-10 mg/kg

  • Administration

    oral

References

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.