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Imeglimin (EMD 387008) Hydrochloride

Synonyms: PXL 008 Hydrochloride, RVT-1501 Hydrochloride, IMEG Hydrochloride

Imeglimin (EMD 387008, IMEG, PXL 008, RVT-1501) Hydrochloride is a new class of oral glucose-lowering agents. Imeglimin normalizes glucose tolerance and insulin sensitivity by preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of HFHSD mice.

Imeglimin (EMD 387008) Hydrochloride Chemical Structure

Imeglimin (EMD 387008) Hydrochloride Chemical Structure

CAS No. 775351-61-6

Purity & Quality Control

Imeglimin (EMD 387008) Hydrochloride Related Products

Biological Activity

Description

Imeglimin (EMD 387008, IMEG, PXL 008, RVT-1501) Hydrochloride is a new class of oral glucose-lowering agents. Imeglimin normalizes glucose tolerance and insulin sensitivity by preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of HFHSD mice.
In vitro
In vitro

Preincubation with Imeglimin (10 mM for 4 h or 100 μM for 24 h) fully prevents tert-butylhydroperoxide (tBH)-induced cell death.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Cell Research Cell lines Human endothelial cells (HMEC-1)
Concentrations 100 μM, 10 mM
Incubation Time 24 h, 4 h
Method

HMEC-1 preincubated with or without Imeglimin (10 mM for 4 h or 100 μM for 24 h) or with CsA (1 μM for 30 min) are ished with PBS before subsequent exposure to 0.5 mM tBH in FBS-free culture medium for 45 min. Cells are then ished with PBS and incubated at 37 °C for 24 h in a complete MCDB medium. Alternatively, cells are exposed to 5.5 mM glucose (control cells) or to 33 mM glucose for 48 h. Cytotoxicity is evaluated with a double-stain system using the Annexin V-Fluoprobes 488 kit combined with propidium iodide.
In Vivo
In vivo

Imeglimin normalizes glucose tolerance and insulin sensitivity by preserving mitochondrial function from oxidative stress and favoring lipid oxidation in liver of high-fat, high-sucrose diet (HFHSD) mice.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Animal Research Animal Models 16-week high-fat, high-sucrose diet (HFHSD) mice
Dosages 200 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03802786 Completed
Hepatic Impairment
Poxel SA
 November 6 2018 Phase 1
NCT03646331 Completed
Bioequivalence
Poxel SA
 September 3 2018 Phase 1
NCT03618316 Completed
Healthy
Poxel SA
 June 19 2018 Phase 1
NCT02373150 Completed
Type 2 Diabetes Mellitus
Poxel SA
 February 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 191.66 Formula

C6H13N5.ClH
CAS No. 775351-61-6 SDF --
Smiles Cl.CC1N=C(N)NC(=N1)N(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 38 mg/mL ( (198.26 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 38 mg/mL

Ethanol : 38 mg/mL


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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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