| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
GKA50 (0.01-100 μM; 24 hours) increases the proliferation of INS-1 cells, with EC50 values between 1 and 2 μM[2]. In INS-1 cells, treatment with GKA50 (1.2 μM+40 μM glucose; 2-4 days) decreases apoptosis caused by prolonged elevated glucose[2]. With an EC50 of 0.022 μM, GKA50 initiates the enzymatic activity of human glucokinase. With an EC50 of 0.065 μM, GKA50 increases insulin secretion in the pancreatic insulinoma cell line, INS-1. Through the regulation of glucokinase and the apoptotic protein BAD, GKA50 lessens chronically high glucose-induced apoptosis[2].
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|---|---|
| ln Vivo |
In an oral glucose tolerance test, GKA50 (1-30 mg/kg; po) significantly lowers glucose levels[1].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: INS-1 cells(starved overnight with 3 μM glucose) Tested Concentrations: 0.01-100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Stimulated cell proliferation in a dose-dependent manner, with EC50 values ranging from 1 to 2 μM. |
| Animal Protocol |
Animal/Disease Models: High-fat-fed obese female Zucker (fa/fa) rats[1]
Doses: 1, 3 , 10, 30 mg/kg Route of Administration: Oral administration Experimental Results: Significant percentage glucose lowering. |
| References |
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| Molecular Formula |
C26H28N2O6.1/4H2O
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|---|---|
| Molecular Weight |
469.01
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| Related CAS # |
GKA50;851884-87-2
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO :~46 mg/mL (~98.08 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1322 mL | 10.6608 mL | 21.3215 mL | |
| 5 mM | 0.4264 mL | 2.1322 mL | 4.2643 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1322 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.
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