Home GPCR & G Protein SGLT inhibitor Remogliflozin etabonate (GSK189075) For research use only.

Remogliflozin etabonate (GSK189075)

Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

Remogliflozin etabonate (GSK189075) Chemical Structure

Remogliflozin etabonate (GSK189075) Chemical Structure

CAS: 442201-24-3

Purity & Quality Control

Batch: S099301 DMSO] 100 mg/mL] false] Ethanol] 25 mg/mL] false] Water] Insoluble] false Purity: 99.67%
99.67

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Signaling Pathway

SGLT Signaling Pathways

SGLT Signaling Pathway

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Biological Activity

Description Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
Targets
hSGLT2 [1]
(Cell-free assay)		 rSGLT2 [1]
(Cell-free assay)		 rSGLT1 [1]
(Cell-free assay)		 hSGLT1 [1]
(Cell-free assay)
1950 nM(Ki) 2140 nM(Ki) 8570 nM(Ki) 43100 nM(Ki)
In vitro
In vitro

Remogliflozin etabonate, a prodrug based on benzylpyrazole glucoside, is metabolized to its active form, remogliflozin, which is a potent and highly selective SGLT2 inhibitor by examining COS-7 cells transiently expressing either high-affinity sodium glucose cotransporter (SGLT1) or SGLT2.[1]
Cell Research Cell lines COS-7 cells
Concentrations --
Incubation Time --
Method

--
In Vivo
In vivo

Treatment with remogliflozin etabonate exhibits antidiabetic efficacy in several rodent models, suggesting that remogliflozin etabonate may be a new and useful drug for the treatment of diabetes.[1]
Animal Research Animal Models male db/db Mice, high-fat diet-fed GK rats
Dosages 5 ml/kg for db/db mice, 0.01, 0.03, or 0.1% for high-fat diet-fed GK rats
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00575159 Completed
Diabetes Mellitus Type 1
GlaxoSmithKline
 March 31 2008 Phase 2
NCT00625859 Completed
Diabetes Mellitus Type 2
GlaxoSmithKline
 January 16 2008 Phase 1
NCT00532610 Completed
Type 2 Diabetes Mellitus|Diabetes Mellitus Type 2
GlaxoSmithKline
 September 2007 Phase 1
NCT00501930 Completed
Type 2 Diabetes Mellitus|Diabetes Mellitus Type 2
GlaxoSmithKline
 April 2007 Phase 1
NCT00501397 Completed
Type 2 Diabetes Mellitus|Diabetes Mellitus Type 2
GlaxoSmithKline
 February 2007 Phase 1
NCT00376038 Completed
Type 2 Diabetes Mellitus|Diabetes Mellitus Type 2
GlaxoSmithKline
 August 2006 Phase 1

Chemical Information & Solubility

Molecular Weight 522.59 Formula

C26H38N2O9
CAS No. 442201-24-3 SDF --
Smiles CCOC(=O)OCC1C(C(C(C(O1)OC2=NN(C(=C2CC3=CC=C(C=C3)OC(C)C)C)C(C)C)O)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (191.35 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


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In vivo
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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.

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.

Handling Instructions

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