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Ipragliflozin (ASP1941) SGLT inhibitor

Name: Ipragliflozin (ASP1941)
Brand: Selleck Chemicals
SKU: S8637
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8637

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.

Chemical Structure

Molecular Weight: 404.45

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.93

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras GPR GluR Prostaglandin Receptor CXCR Adenosine Receptor P2 Receptor CCR Angiotensin Receptor Hedgehog/Smoothened S1P Receptor PKA Cannabinoid Receptor cAMP Glucagon Receptor Opioid Receptor Sigma Receptor PAR Endothelin Receptor LTR Neurokinin Receptor Guanylate Cyclase PKG LPA Receptor OX Receptor
Related Products	Sotagliflozin Phlorizin Phloretin (RJC 02792)

Chemical Information, Storage & Stability

Molecular Weight	404.45	Formula	C₂₁H₂₁FOS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	761423-87-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C2C(=C1)C=C(S2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)F

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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 1 40%PEG300 2 5%Tween80 3 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 1 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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	mouse SGLT2 ^[2] (cell-free) 5.64 nM rat SGLT2 ^[2] (cell-free) 6.73 nM hSGLT2 ^[1] (cell-free) 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].
References	https://pubmed.ncbi.nlm.nih.gov/22507206/ https://pubmed.ncbi.nlm.nih.gov/22139434/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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