| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
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.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| References |
J Biomol Struct Dyn.2019 Jan 11:1-15. doi: 10.1080/07391102.2019.1567391.
|
||
| Additional Infomation |
LY2608204 has been used in trials studying the treatment of Diabetes Mellitus, Type 2.
|
| Molecular Formula |
C28H37N3O3S3
|
|
|---|---|---|
| Molecular Weight |
559.81
|
|
| Exact Mass |
559.199
|
|
| CAS # |
1234703-40-2
|
|
| Related CAS # |
1234703-40-2;Globalagliatin HCl;
|
|
| PubChem CID |
46832368
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.4±0.1 g/cm3
|
|
| Index of Refraction |
1.658
|
|
| LogP |
4.97
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
7
|
|
| Rotatable Bond Count |
10
|
|
| Heavy Atom Count |
37
|
|
| Complexity |
903
|
|
| Defined Atom Stereocenter Count |
2
|
|
| SMILES |
C1CCC(CC1)[C@@H]2C[C@@]2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6
|
|
| InChi Key |
QIIVJLHCZUTGSD-CUBQBAPOSA-N
|
|
| InChi Code |
InChI=1S/C28H37N3O3S3/c32-26(30-27-29-19-25(36-27)35-17-16-31-14-4-5-15-31)28(18-24(28)20-6-2-1-3-7-20)21-8-10-22(11-9-21)37(33,34)23-12-13-23/h8-11,19-20,23-24H,1-7,12-18H2,(H,29,30,32)/t24-,28-/m0/s1
|
|
| Chemical Name |
(1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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 (In Vitro) |
|
|||
|---|---|---|---|---|
| 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. View More
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. Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 30 mg/mL |
| 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.
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA