Globalagliatin

Globalagliatin (LY2608204) is an orally active glucokinase (GK) activator with an EC50 of 42 nM. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with an EC50 of 579 nM. Globalagliatin targets both pancreatic β-cells and hepatocytes. Globalagliatin is promising for research of type 2 diabetes[1][2][3].

Product Specifications

CAS Number

[1234703-40-2]

Product Name Alternative

LY2608204; SY-004

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Glucokinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/LY2608204.html

Purity

98.0

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C([C@@]1(C2=CC=C(S(=O)(C3CC3)=O)C=C2)[C@H](C4CCCCC4)C1)NC5=NC=C(SCCN6CCCC6)S5

Molecular Formula

C28H37N3O3S3

Molecular Weight

559.81

Precautions

H302, H315, H319, H335

References & Citations

[1]Zheng S, et al. Safety, Pharmacokinetics, and Pharmacodynamics of Globalagliatin, a Glucokinase Activator, in Chinese Patients with Type 2 Diabetes Mellitus: A Randomized, Phase Ib, 28-day Ascending Dose Study. Clin Drug Investig. 2020 Dec;40 (12) :1155-1166.|[2]Xu M, et al. Unveiling the Influence of a High-Fat Meal on the Pharmacokinetics of Oral Globalagliatin, A Glucokinase Activator, in Healthy Chinese Volunteers. Drugs R D. 2024 Mar;24 (1) :41-50.|[3]Li P, et al. Clinical investigation of glucokinase activators for the restoration of glucose homeostasis in diabetes. J Diabetes. 2024 May;16 (5) :e13544.|[4]Liao M, et al. Oridonin inhibits DNMT3A R882 mutation-driven clonal hematopoiesis and leukemia by inducing apoptosis and necroptosis. Cell Death Discov. 2021 Oct 18;7 (1) :297.