LY2608204

Alias: LY-2608204; LY 2608204; LY2608204
Cat No.:V2010 Purity: ≥98%
LY2608204, an investigational drug, is a novel and potent activator of glucokinase (GK) with EC50 of 42 nM.
LY2608204 Chemical Structure CAS No.: 1234703-40-2
Product category: Carbohydrate Metabolism
This product is for research use only, not for human use. We do not sell to patients.
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10mg
25mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

LY2608204, an investigational drug, is a novel and potent activator of glucokinase (GK) with EC50 of 42 nM. It activates glucokinase (GK) and has shown the novel and potent stimulant of glucokinase (GK) with the EC50 value of 42nM at lower glucose concentrations. In addition, LY2608204 has been reported to activate glucose metabolism with the EC50 value of 579nM in rat insulinoma INS1-E cell lines. Apart from these, LY2608204 has been revealed to lower plasma glucose in a dose-dependent fashion at the levels of fasted and postprandial. LY-2608204 entered clinical trials in 2010 for treat Patients With Type 2 Diabetes.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: 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.

ln 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.
Animal Protocol
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; 1, 3, 6, 10, 20 and 30 mg/kg; Orally, rats are given a 2 g/kg oral glucose bolus 2 hours after LY2608204 administration.
Male Wistar rats at a weight of 225-250 g
References
2019 Jan 11:1-15. doi: 10.1080/07391102.2019.1567391.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H37N3O3S3
Molecular Weight
559.81
CAS #
1234703-40-2
Related CAS #
1234703-40-2;Globalagliatin HCl;
SMILES
O=C([C@@]1(C2=CC=C(S(=O)(C3CC3)=O)C=C2)[C@H](C4CCCCC4)C1)NC5=NC=C(SCCN6CCCC6)S5
Synonyms
LY-2608204; LY 2608204; LY2608204
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:112 mg/mL (200.1 mM)
Water:<1 mg/mL
Ethanol:35 mg/mL (62.5 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 30 mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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