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Ipragliflozin L-Proline SGLT inhibitor

Name: Ipragliflozin L-Proline
SKU: S0994
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0994

Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively.

Chemical Structure

Molecular Weight: 519.58

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

Quality Control

Batch: S099401 DMSO]35 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false Purity: 99.37%

99.37

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) Tofogliflozin(CSG 452) Ipragliflozin (ASP1941) Swertisin KGA-2727 Mizagliflozin (KWA 0711) Bexagliflozin (EGT1442)

Chemical Information, Storage & Stability

Molecular Weight	519.58	Formula	C₂₆H₃₀FNO₇S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	951382-34-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC(NC1)C(=O)O.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 : 35 mg/mL (67.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 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.	6mg/ml (11.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 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.

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 ^[1] (Cell-free assay) 5.64 nM rat SGLT2 ^[1] (Cell-free assay) 6.73 nM human SGLT2 ^[1] (Cell-free assay) 7.38 nM
References	[1] 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
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

Tech Support

Handling Instructions

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