Imeglimin - CAS 775351-65-0
Catalog number:
775351-65-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C6H13N5
Molecular Weight:
155.2
COA:
Inquire
Targets:
AMPK
Description:
Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins. It has been shown to act on the liver, muscle and pancreatic β-cells to uniquely target the key defects of type 2 diabetes.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
EMD 387008
MSDS:
Inquire
1.Imeglimin, a novel glimin oral antidiabetic, exhibits a good efficacy and safety profile in type 2 diabetic patients.
Pirags V1, Lebovitz H, Fouqueray P. Diabetes Obes Metab. 2012 Sep;14(9):852-8. doi: 10.1111/j.1463-1326.2012.01611.x. Epub 2012 May 16.
AIMS: Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins. It has been shown to act on the liver, muscle and pancreatic β-cells to uniquely target the key defects of type 2 diabetes. Two studies were performed to compare the safety and efficacy of imeglimin with metformin and placebo on glycaemic control in type 2 diabetes patients.
2.The efficacy and safety of imeglimin as add-on therapy in patients with type 2 diabetes inadequately controlled with sitagliptin monotherapy.
Fouqueray P1, Pirags V2, Diamant M3, Schernthaner G4, Lebovitz HE5, Inzucchi SE6, Bailey CJ7. Diabetes Care. 2014 Jul;37(7):1924-30. doi: 10.2337/dc13-2349. Epub 2014 Apr 10.
OBJECTIVE: This 12-week study assessed the efficacy and tolerability of imeglimin as add-on therapy to the dipeptidyl peptidase-4 inhibitor sitagliptin in patients with type 2 diabetes inadequately controlled with sitagliptin monotherapy.
3.Imeglimin: A Potential New Multi-Target Drug for Type 2 Diabetes.
Vuylsteke V1, Chastain LM, Maggu GA, Brown C. Drugs R D. 2015 Sep;15(3):227-32. doi: 10.1007/s40268-015-0099-3.
Imeglimin is a novel agent currently in development to treat type 2 diabetes. Laboratory studies have demonstrated that it has the potential to impact the three main pathophysiologic components of type 2 diabetes: impaired glucose uptake by muscle tissue, excess hepatic gluconeogenesis, and increased beta-cell apoptosis. Preliminary human studies that have been published within the last 2 years demonstrate that imeglimin improves hemoglobin A1c and fasting plasma glucose similarly when compared with metformin and with sitagliptin. There has also been a low incidence of adverse effects, especially hypoglycemia, reported in these early human studies. Currently, imeglimin is lacking long-term evidence to demonstrate any effects on its cardiovascular safety, and data on morbidity and mortality, though some studies are currently in progress. There is great potential for imeglimin, if FDA approved, to play a significant role in the type 2 diabetes management algorithm.
4.Imeglimin normalizes glucose tolerance and insulin sensitivity and improves mitochondrial function in liver of a high-fat, high-sucrose diet mice model.
Vial G1, Chauvin MA2, Bendridi N2, Durand A2, Meugnier E2, Madec AM2, Bernoud-Hubac N2, Pais de Barros JP3, Fontaine É4, Acquaviva C5, Hallakou-Bozec S6, Bolze S6, Vidal H7, Rieusset J7. Diabetes. 2015 Jun;64(6):2254-64. doi: 10.2337/db14-1220. Epub 2014 Dec 31.
Imeglimin is the first in a new class of oral glucose-lowering agents currently in phase 2b development. Although imeglimin improves insulin sensitivity in humans, the molecular mechanisms are unknown. This study used a model of 16-week high-fat, high-sucrose diet (HFHSD) mice to characterize its antidiabetic effects. Six-week imeglimin treatment significantly decreased glycemia, restored normal glucose tolerance, and improved insulin sensitivity without modifying organs, body weights, and food intake. This was associated with an increase in insulin-stimulated protein kinase B phosphorylation in the liver and muscle. In liver mitochondria, imeglimin redirects substrate flows in favor of complex II, as illustrated by increased respiration with succinate and by the restoration of respiration with glutamate/malate back to control levels. In addition, imeglimin inhibits complex I and restores complex III activities, suggesting an increase in fatty acid oxidation, which is supported by an increase in hepatic 3-hydroxyacetyl-CoA dehydrogenase activity and acylcarnitine profile and the reduction of liver steatosis.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related AMPK Products


CAS 1219168-18-9 Dorsomorphin 2HCl

Dorsomorphin 2HCl
(CAS: 1219168-18-9)

CAS 866405-64-3 Dorsomorphin

Dorsomorphin
(CAS: 866405-64-3)

Dorsomorphin has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase) (Ki = 109 nM), induced by AICAR and metformin. It ...

CAS 1613724-42-7 HTH-01-015

HTH-01-015
(CAS: 1613724-42-7)

HTH-01-015 is a potent and selective inhibitor of NUAK1 with IC50 of 100 nM, does not significantly inhibit NUAK2 (IC50 of >10 μM).

CAS 775351-61-6 Imeglimin hydrochloride

Imeglimin hydrochloride
(CAS: 775351-61-6)

Imeglimin hydrochloride is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins. It has been shown to act on the live...

SC-III3
(CAS: 1660110-65-5)

SC-III3 is a scopoletin derivative and has been found to induce the autophagy of hepatoma HepG2 cells so that could be significant in anticancer studies.

Ampkinone
(CAS: 1233082-79-5)

Ampkinone, an AMPK activitor, has been found to have potential effect in the treatment of diabete and obesity. IC50: 4.3 uM(EC50).

CAS 723249-01-2 ZLN024

ZLN024
(CAS: 723249-01-2)

ZLN024 is a novel AMPK allosteric activator and activates α1β1γ1 and α2β1γ1 by around 2–2.5 fold. It activated AMPK in L6 myotubes and stimulated glucose uptake...

CAS 51415-02-2 Chikusetsu saponin IVa

Chikusetsu saponin IVa
(CAS: 51415-02-2)

Chikusetsusaponin IVa is a novel AMPK activator could be useful for the treatment of T2DM or other metabolic disorders.

CAS 775351-65-0 Imeglimin

Imeglimin
(CAS: 775351-65-0)

Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins. It has been shown to act on the liver, muscle and ...

CAS 844499-71-4 A769662

A769662
(CAS: 844499-71-4)

CAS 1273323-67-3 YLF-466D

YLF-466D
(CAS: 1273323-67-3)

YLF466D activated recombinant human α1β1γ1, α2β1γ1 and rat liver AMPK. It also activated AMPK α-subunit truncations containing an autoinhibitory domain(AID) and...

CAS 1214265-58-3 WZ4003

WZ4003
(CAS: 1214265-58-3)

WZ4003 exhibits a high, specific affinity to the L858R/T790M mutant EGFR, while a significantly reduced cellular IC50 against T790M containing Ba/F3 cells.

CAS 125911-68-4 SAMS

SAMS
(CAS: 125911-68-4)

SAMS peptide, a synthetic peptide substrate for AMPK based on the sequence around Ser79 on acetyl-CoA carboxylase, is more selective for the kinase than acetyl ...

CAS 681006-28-0 AICAR phosphate

AICAR phosphate
(CAS: 681006-28-0)

AICAR phosphate, is an AMP-activated protein kinase activator, which is used for the treatment of acute lymphoblastic leukemia and may have applications in trea...

CAS 2627-69-2 Acadesine

Acadesine
(CAS: 2627-69-2)

Acadesine is a 5-aminoimidazole-4-carboxamide (AICA) riboside, a purine nucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic act...

CAS 738606-46-7 ETC-1002

ETC-1002
(CAS: 738606-46-7)

ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule and is activator of hepatic AMP-activated protein kinase (AMPK)....

Chemical Structure

CAS 775351-65-0 Imeglimin

Quick Inquiry

Verification code

Featured Items