Home Metabolism Carbohydrate Metabolism modulator LY2608204

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LY2608204 Carbohydrate Metabolism modulator

Cat.No.S2155

LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.
LY2608204 Carbohydrate Metabolism modulator Chemical Structure

Chemical Structure

Molecular Weight: 559.81

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Quality Control

Batch: Purity: 99.74%
99.74

Solubility

In vitro
Batch:

DMSO : 112 mg/mL (200.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 35 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.

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Chemical Information, Storage & Stability

Molecular Weight 559.81 Formula

C28H37N3O3S3

 Storage (From the date of receipt)
CAS No. 1234703-40-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CCC(CC1)C2CC2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6

Mechanism of Action

Targets/IC50/Ki
glucokinase
42 nM(EC50)
In vitro
LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. This compound also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.
In vivo
LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg dose. The in vivo blood brain barrier permeability of this compound results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01408095 Withdrawn
Diabetes Mellitus Type 2
Eli Lilly and Company
 September 2011 Phase 2

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