Home Metabolism Carbohydrate Metabolism modulator LY2608204 For research use only.

LY2608204

LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.

LY2608204 Chemical Structure

LY2608204 Chemical Structure

CAS No. 1234703-40-2

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Biological Activity

Description LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.
Targets
glucokinase [1]
42 nM(EC50)
In vitro
In vitro LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM. [1]
In Vivo
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 LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 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. [1]
Animal Research Animal Models Male Wistar rats at a weight of 225-250 g
Dosages 1, 3, 6, 10, 20 and 30 mg/kg
Administration Orally, rats are given a 2 g/kg oral glucose bolus 2 hours after LY2608204 administration.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01408095 Withdrawn
Diabetes Mellitus Type 2
Eli Lilly and Company
 September 2011 Phase 2

Chemical Information & Solubility

Molecular Weight 559.81 Formula

C28H37N3O3S3
CAS No. 1234703-40-2 SDF Download LY2608204 SDF
Smiles C1CCC(CC1)C2CC2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 112 mg/mL ( (200.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh 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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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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