LY2608204

Catalog No.S2155 Batch:S215501

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Technical Data

Formula

C28H37N3O3S3
Molecular Weight 559.81 CAS No. 1234703-40-2
Solubility (25°C)* In vitro DMSO 112 mg/mL (200.06 mM)
Ethanol 35 mg/mL (62.52 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Animal Study:[1]
  • 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.

Customer Product Validation

Data from [Data independently produced by , , Nat Commun, 2016, 7:11463]

Selleck's LY2608204 has been cited by 2 publications

Identification of mangiferin as a potential Glucokinase activator by structure-based virtual ligand screening [Min Q Sci Rep, 2017, 7:44681] PubMed: 28317897
Generation of stem cell-derived β-cells from patients with type 1 diabetes. [ Nat Commun, 2016, 7:11463] PubMed: 27163171

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.