| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
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| Other Sizes |
| Targets |
WAY-615145 specifically targets glucokinase (GCK), a member of the hexokinase family that catalyzes the phosphorylation of glucose to glucose-6-phosphate. Glucokinase is predominantly expressed in the liver, pancreatic beta cells, and specific regions of the hypothalamus, where it functions as a glucose sensor. In pancreatic beta cells, glucokinase plays a critical role in glucose-stimulated insulin secretion by sensing changes in extracellular glucose concentration and regulating the rate of glucose metabolism. In the liver, glucokinase regulates glucose uptake and glycogen synthesis in response to postprandial glucose levels. Mutations in the glucokinase gene are associated with maturity-onset diabetes of the young (MODY), highlighting the importance of this enzyme in glucose homeostasis. By activating glucokinase, WAY-615145 enhances glucose phosphorylation and downstream metabolic pathways.
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| ln Vitro |
In vitro, WAY-615145 activates glucokinase enzymatic activity. The compound is designed to bind to an allosteric site on glucokinase, stabilizing the enzyme in its active conformation and increasing its affinity for glucose. By activating glucokinase, the compound enhances the conversion of glucose to glucose-6-phosphate, promoting glucose metabolism in target cells. The compound's activity has been characterized in enzymatic assays using recombinant glucokinase. Specific EC50 values and detailed in vitro activity data are available from the primary literature describing the compound. WAY-615145 is used as a research tool for studying glucokinase biology and for validating glucokinase as a therapeutic target for diabetes.
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| ln Vivo |
In vivo activity of WAY-615145 has been investigated in preclinical models of diabetes. By activating glucokinase, the compound is expected to lower blood glucose levels through increased glucose utilization in the liver and enhanced insulin secretion from pancreatic beta cells. Glucokinase activators have been shown to improve glucose tolerance and reduce fasting blood glucose in animal models of type 2 diabetes. Specific in vivo efficacy data for WAY-615145, including effects on blood glucose levels, glucose tolerance, and insulin secretion, is available from the primary literature. The compound is typically administered orally in these studies, consistent with the oral activity of other glucokinase activators.
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| Enzyme Assay |
The enzymatic activity of WAY-615145 against glucokinase is assessed using standard kinase activity assays. Recombinant human glucokinase is incubated with glucose, ATP, and a glucose-6-phosphate dehydrogenase-coupled system in the presence of varying concentrations of the test compound. The production of glucose-6-phosphate is monitored by measuring the reduction of NADP⁺ to NADPH at 340 nm. The compound's ability to activate glucokinase is expressed as the concentration required for 50% activation (EC50). Selectivity for glucokinase over other hexokinase isoforms can be assessed using similar assays with recombinant hexokinase isoforms.
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| Cell Assay |
Cellular assays for WAY-615145 are performed using cells that express glucokinase, such as hepatocytes (e.g., HepG2 cells) or pancreatic beta cells (e.g., MIN6 or INS-1 cells). Cells are treated with varying concentrations of the compound, and glucose metabolism is assessed by measuring glucose consumption, glucose-6-phosphate production, or lactate production. In pancreatic beta cells, insulin secretion is measured by ELISA or radioimmunoassay following glucose stimulation. In hepatocytes, glycogen synthesis can be assessed by measuring the incorporation of radiolabeled glucose into glycogen. The compound's effects on glucose metabolism and insulin secretion are quantified.
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| Animal Protocol |
In vivo studies of WAY-615145 are conducted in rodent models of diabetes, such as db/db mice or streptozotocin-induced diabetic rats. The compound is typically administered orally via gavage. Blood glucose levels are measured at various time points post-administration using glucometers. Glucose tolerance tests are performed by administering a glucose challenge and measuring blood glucose levels over time. Insulin levels are measured by ELISA. Body weight and food intake are monitored throughout the study. The compound is formulated in vehicles such as 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of WAY-615145 (molecular weight 286.39, molecular formula C16H18N2OS) have been characterized. The compound is soluble in DMSO at 10 mM and is typically formulated in suitable vehicles for in vivo administration. For in vivo administration, the compound can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline. Storage recommendations include powder storage at -20°C for up to 3 years and solution storage at -80°C for 1 year. Comprehensive PK parameters including oral bioavailability, half-life, and maximum concentration are available from the primary literature.
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| Toxicity/Toxicokinetics |
WAY-615145 is intended for research use only and is not approved for human therapeutic applications. Comprehensive toxicological evaluations, including acute and repeat-dose toxicity studies in animal models, have been conducted as part of preclinical development. Glucokinase activators have been associated with potential side effects including hypoglycemia and hepatic steatosis, and these effects would be carefully evaluated in toxicology studies. Standard safety pharmacology assessments would include evaluation of effects on glucose homeostasis, liver function, and lipid metabolism.
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| Additional Infomation |
WAY-615145 is a research-grade compound used as a pharmacological tool for studying glucokinase biology and for validating glucokinase as a therapeutic target for diabetes. Glucokinase is a key enzyme in glucose metabolism that functions as a glucose sensor in pancreatic beta cells and regulates glucose uptake in the liver. Glucokinase activators are being investigated as potential therapeutic agents for type 2 diabetes mellitus, as they can enhance glucose utilization and lower blood glucose levels. WAY-615145 is also known by synonyms including Z56935488, WAY615145, Oprea1_053963, and CHEMBL1821902. The compound is available with purity specifications for research use.
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| Molecular Formula |
C16H18N2OS
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| Molecular Weight |
286.391922473907
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| Exact Mass |
286.11
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| Elemental Analysis |
C, 67.10; H, 6.34; N, 9.78; O, 5.59; S, 11.19
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| CAS # |
536736-95-5
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| PubChem CID |
2471840
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
324
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(CC1)C2=CSC(=N2)NC(=O)C3=CC=CC=C3
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| InChi Key |
XDROZDYEXSKYNN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N2OS/c19-15(13-9-5-2-6-10-13)18-16-17-14(11-20-16)12-7-3-1-4-8-12/h2,5-6,9-12H,1,3-4,7-8H2,(H,17,18,19)
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| Chemical Name |
N-(4-cyclohexylthiazol-2-yl)benzamide
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| Synonyms |
Oprea1_053963; CHEMBL1821902; AKOS001063992; WAY-615145; Z56935488; WAY 615145; WAY615145
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.4917 mL | 17.4587 mL | 34.9174 mL | |
| 5 mM | 0.6983 mL | 3.4917 mL | 6.9835 mL | |
| 10 mM | 0.3492 mL | 1.7459 mL | 3.4917 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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