LY2608204

Catalog No.S2155

LY2608204 Chemical Structure

Molecular Weight(MW): 559.81

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

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Cited by 1 Publication

1 Customer Review

  • ELISA measurements of secreted human insulin at 2 and 20 mM glucose for a subset of cell lines treated with the anti-diabetic drugs Tolbutamide (sulfonylurea), Liraglutide (GLP-1 R agonist) and LY2608204 (GCK activator). n = 4 measurements for each line. *P<0.05 and **P<0.01 comparing drug treatment with no treatment at the same glucose concentration (two-sided unpaired t-test). Data shown as mean±s.e.m. Samples taken after 10-17 days in Stage 6. Act A, activin A; Alk5i, Alk5 receptor inhibitor II; CHIR, CHIR9901; KGF, keratinocyte growth factor; LDN, LDN193189; PdbU, phorbol 12,13-dibutyrate; RA, retinoic acid; T3, triiodothyronine; Y, Y27632.

    Nat Commun, 2016, 7:11463. LY2608204 purchased from Selleck.

Purity & Quality Control

Choose Selective Carbohydrate Metabolism Inhibitors

Biological Activity

Description LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.
Targets
glucokinase [1]
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. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM. [1]

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]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Male Wistar rats at a weight of 225-250 g
  • Formulation: LY2608204 is suspended in a 1:1 mixture of solutol/ethanol in a bath sonicator (10% of total volume). The obtained suspension is then diluted with 9 volumes of 10% aqueous solutol solution.
  • 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.
    (Only for Reference)

References

Solubility (25°C)

In vitro DMSO 112 mg/mL (200.06 mM)
Ethanol 35 mg/mL (62.52 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 559.81
Formula

C28H37N3O3S3

CAS No. 1234703-40-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01408095 Withdrawn Diabetes Mellitus Type 2 Eli Lilly and Company September 2011 Phase 2
NCT01408095 Withdrawn Diabetes Mellitus Type 2 Eli Lilly and Company September 2011 Phase 2
NCT01313286 Completed Healthy Volunteers Eli Lilly and Company March 2011 Phase 1
NCT01313286 Completed Healthy Volunteers Eli Lilly and Company March 2011 Phase 1
NCT01247363 Completed Diabetes Mellitus Type 2 Eli Lilly and Company November 2010 Phase 1
NCT01247363 Completed Diabetes Mellitus Type 2 Eli Lilly and Company November 2010 Phase 1

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID