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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cadisegliatin targets glucokinase (GK), an enzyme that plays a key role in glucose sensing and metabolism. GK is primarily expressed in the liver and pancreatic β-cells. By activating GK, the compound increases glucose phosphorylation and uptake in the liver, reducing blood glucose levels. Its liver-selectivity is intended to avoid the risk of hypoglycemia associated with non-selective GK activators.
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| ln Vitro |
Cadisegliatin (TTP-399) raises the recruitment of auxiliary hepatocytes; its effects on medium elimination and glycogen EC50 values (2.39) and 2.64 μM, respectively, are enhanced at 15 nM [2].
In vitro, Cadisegliatin activates human GK with EC50 values of 304 nM at 15 mM glucose and 762 nM at 5 mM glucose. It increases the recruitment of auxiliary hepatocytes, with EC50 values of 2.39 µM and 2.64 µM for medium elimination and glycogen effects, respectively. These data demonstrate its potent and glucose-dependent activation of GK. |
| ln Vivo |
TTP399 (200 mg/kg, passage, passage) had little effect on fasting antibiotics and insulin [2]. TTP399 (75 or 150 mg/kg daily for 4 weeks) improves ob/ob electrode models TTP399 (50 mg/kg daily for 13 weeks) is effective during the sidewall backlight tolerance test (OGTT) in a minipig model Reduce stair short circuits[2].
In vivo, Cadisegliatin has antihyperglycemic activity. As a liver-selective GK activator, it lowers blood glucose without the risk of hypoglycemia. Specific in vivo efficacy data, such as effects in animal models of diabetes, are not detailed in the available sources. |
| Enzyme Assay |
A cell-free assay for Cadisegliatin involves measuring its activation of glucokinase enzymatic activity. Recombinant human GK is incubated with glucose and ATP in the presence of varying concentrations of the compound. The production of glucose-6-phosphate is measured, and the EC50 is calculated. For Cadisegliatin, the EC50 values are 304 nM at 15 mM glucose and 762 nM at 5 mM glucose.
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| Cell Assay |
Cellular assays for Cadisegliatin would typically involve measuring its effects on glucose metabolism in hepatocytes. Cells are treated with the compound, and glucose uptake, glycogen synthesis, and glucose production are measured. The compound's ability to increase glucose phosphorylation and metabolism confirms its GK-activating activity.
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| Animal Protocol |
Animal/Disease Models: ob/ob mouse model [2]
Doses: 75 or 150 mg/kg Route of Administration: 75 or 150 mg/kg daily for 4 weeks Experimental Results: diminished HbA1c, blood glucose concentration, lactate concentration, and hepatic expression of glycogen library. The highest dose can improve blood lipids, reduce plasma and liver TG concentrations and increase body weight. Animal/Disease Models: Göttingen mini-pig [2] Doses: 50 mg/kg Route of Administration: 50 mg/kg per day for 13 weeks Experimental Results: Elimination of blood glucose fluctuations in mini-pig. In vivo animal experiments for Cadisegliatin are not described in the available sources. As a compound being developed for type 2 diabetes, it would be evaluated in animal models of diabetes. However, no specific protocols or data are provided. |
| ADME/Pharmacokinetics |
Cadisegliatin is an orally active compound. Specific pharmacokinetic parameters, such as half-life and bioavailability, are not provided in the available sources. Its IUPAC name is 2-((2-(3-cyclohexyl-3-((1R,4R)-4-propoxycyclohexyl)ureido)thiazol-5-yl)thio)acetic acid.
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| Toxicity/Toxicokinetics |
Toxicity data for Cadisegliatin are not provided in the available sources. As a research compound, it is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be observed.
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| References | |
| Additional Infomation |
Cadisegliatin (CAS: 859525-02-3) is a potential, orally active, liver-selective glucokinase activator. It is also known as TTP-399. The compound has antihyperglycemic activity and is being studied for the treatment of type 2 diabetes. It is not an approved drug and is strictly for research purposes.
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| Molecular Formula |
C21H33N3O4S2
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|---|---|
| Molecular Weight |
455.634423017502
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| Exact Mass |
455.191
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| CAS # |
859525-02-3
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| PubChem CID |
54673176
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| Appearance |
Off-white to pale purple solid powder
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| LogP |
5.297
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(O)(=O)CSC1SC(NC(N(C2CCCCC2)[C@@H]2CC[C@@H](OCCC)CC2)=O)=NC=1
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~274.35 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 | 2.1948 mL | 10.9738 mL | 21.9476 mL | |
| 5 mM | 0.4390 mL | 2.1948 mL | 4.3895 mL | |
| 10 mM | 0.2195 mL | 1.0974 mL | 2.1948 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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