For research use only.

Catalog No.S2155

2 publications

LY2608204 Chemical Structure

CAS No. 1234703-40-2

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

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10mM (1mL in DMSO) EUR 589 In stock
EUR 265 In stock
EUR 363 In stock
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Selleck's LY2608204 has been cited by 2 publications

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  • 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.

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Biological Activity

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


Animal Research:[1]
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  • 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.
    (Only for Reference)


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


CAS No. 1234703-40-2
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC(CC1)C2CC2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID