Globalagliatin
Based on 1 publication(s) in Google Scholar
Globalagliatin (LY2608204) is an orally active glucokinase (GK) activator with an EC50 of 42 nM. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with an EC50 of 579 nM. Globalagliatin targets both pancreatic β-cells and hepatocytes. Globalagliatin is promising for research of type 2 diabetes.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 1234703-40-2
- Formula: C28H37N3O3S3
- Molecular Weight:559.81
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Publications Citing Use of MedChemExpress (MCE) Globalagliatin
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Biological Activity
Globalagliatin (LY2608204) displays no selective inhibitory effect under 5 µM in DNMT3A R882H cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1234703-40-2
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Appearance Solid
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Molecular Weight 559.81
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Formula C28H37N3O3S3
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Color White to off-white
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SMILES
O=C([C@@]1(C2=CC=C(S(=O)(C3CC3)=O)C=C2)[C@H](C4CCCCC4)C1)NC5=NC=C(SCCN6CCCC6)S5
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Synonyms
LY2608204; SY-004
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep
Brain endothelial PTEN/AKT/NEDD4-2/MFSD2A axis regulates blood-brain barrier permeability. [Abstract]2021 Jul 6;36(1):109327. PMID: 34233198
Solvent & Solubility
DMSO : ≥ 100 mg/mL (178.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Zheng S, et al. Safety, Pharmacokinetics, and Pharmacodynamics of Globalagliatin, a Glucokinase Activator, in Chinese Patients with Type 2 Diabetes Mellitus: A Randomized, Phase Ib, 28-day Ascending Dose Study. Clin Drug Investig. 2020 Dec;40(12):1155-1166. [Content Brief]
[2]. Xu M, et al. Unveiling the Influence of a High-Fat Meal on the Pharmacokinetics of Oral Globalagliatin, A Glucokinase Activator, in Healthy Chinese Volunteers. Drugs R D. 2024 Mar;24(1):41-50. [Content Brief]
[3]. Li P, et al. Clinical investigation of glucokinase activators for the restoration of glucose homeostasis in diabetes. J Diabetes. 2024 May;16(5):e13544. [Content Brief]
[4]. Liao M, et al. Oridonin inhibits DNMT3A R882 mutation-driven clonal hematopoiesis and leukemia by inducing apoptosis and necroptosis. Cell Death Discov. 2021 Oct 18;7(1):297. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7863 mL | 8.9316 mL | 17.8632 mL | 44.6580 mL |
| 5 mM | 0.3573 mL | 1.7863 mL | 3.5726 mL | 8.9316 mL | |
| 10 mM | 0.1786 mL | 0.8932 mL | 1.7863 mL | 4.4658 mL | |
| 15 mM | 0.1191 mL | 0.5954 mL | 1.1909 mL | 2.9772 mL | |
| 20 mM | 0.0893 mL | 0.4466 mL | 0.8932 mL | 2.2329 mL | |
| 25 mM | 0.0715 mL | 0.3573 mL | 0.7145 mL | 1.7863 mL | |
| 30 mM | 0.0595 mL | 0.2977 mL | 0.5954 mL | 1.4886 mL | |
| 40 mM | 0.0447 mL | 0.2233 mL | 0.4466 mL | 1.1165 mL | |
| 50 mM | 0.0357 mL | 0.1786 mL | 0.3573 mL | 0.8932 mL | |
| 60 mM | 0.0298 mL | 0.1489 mL | 0.2977 mL | 0.7443 mL | |
| 80 mM | 0.0223 mL | 0.1116 mL | 0.2233 mL | 0.5582 mL | |
| 100 mM | 0.0179 mL | 0.0893 mL | 0.1786 mL | 0.4466 mL |
Globalagliatin Related Classifications
HY-13529 Related Classifications
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