1. Metabolic Enzyme/Protease
  2. Glucokinase
  3. LY2608204

LY2608204 

Cat. No.: HY-13529 Purity: 98.18%
Handling Instructions

LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM.

For research use only. We do not sell to patients.

LY2608204 Chemical Structure

LY2608204 Chemical Structure

CAS No. : 1234703-40-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 236 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 990 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM. IC 50 value: 42 nM (EC50) Target: glucokinase 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. 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. Clinical trail:

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (178.63 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7863 mL 8.9316 mL 17.8632 mL
5 mM 0.3573 mL 1.7863 mL 3.5726 mL
10 mM 0.1786 mL 0.8932 mL 1.7863 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
Molecular Weight

559.81

Formula

C₂₈H₃₇N₃O₃S₃

CAS No.

1234703-40-2

SMILES

O=C([[email protected]@]1(C2=CC=C(S(=O)(C3CC3)=O)C=C2)[[email protected]](C4CCCCC4)C1)NC5=NC=C(SCCN6CCCC6)S5

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
LY2608204
Cat. No.:
HY-13529
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LY2608204

Cat. No.: HY-13529