Cadisegliatin
Based on 1 Customer Validation
Cadisegliatin (TTP-399) is a potential, orally active liver-selective glucokinase (GK) activator. Cadisegliatin has antihyperglycaemic activity. Cadisegliatin can be used for the research of type 2 diabetes.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 859525-02-3
- Formula: C21H33N3O4S2
- Molecular Weight:455.63
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Biological Activity
Cadisegliatin (TTP-399) increases glucose metabolism in rat hepatocytes, the EC50 values of lactate and glycogen in 15 nM glucose are 2.39 μM and 2.64 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TTP399 (75 or 150 mg/kg, per day, for 4 weeks) improves glucose homeostasis in ob/ob mouse model[2].
TTP399 (50 mg/kg, per day, for 13 weeks) is effective in reducing plasma glucose during an oral glucose tolerance test (OGTT) in minipigs model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nondiabetic fasted rats[2]
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Dosage:200 mg/kg
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Administration:200 mg/kg, per os (p.o.)
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Result:Did not change the insulin and glucose concentrations in plasma.
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Animal Model:ob/ob mouse model[2]
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Dosage:75 or 150 mg/kg
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Administration:75 or 150 mg/kg, per day, for 4 weeks
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Result:Reduced the expression of HbA1c, blood glucose concentrations, lactate concentrations and liver glycogen depots.
Improved the lipid profile, reduced plasma, liver TG concentrations and the weight gain at the highest dose.
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Animal Model:Gottingen minipigs[2]
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Dosage:50 mg/kg
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Administration:50 mg/kg, per day, for 13 weeks
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Result:Eliminated the blood glucose excursion in Minipigs.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 859525-02-3
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Appearance Solid
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Molecular Weight 455.63
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Formula C21H33N3O4S2
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Color Off-white to pale purple
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SMILES
OC(CSC1=CN=C(S1)NC(N(C2CCCCC2)[C@H]3CC[C@@H](CC3)OCCC)=O)=O
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Synonyms
TTP-399
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL (274.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (21.95 mM); Suspended solution; Need ultrasonic
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1948 mL | 10.9738 mL | 21.9476 mL | 54.8691 mL |
| 5 mM | 0.4390 mL | 2.1948 mL | 4.3895 mL | 10.9738 mL | |
| 10 mM | 0.2195 mL | 1.0974 mL | 2.1948 mL | 5.4869 mL | |
| 15 mM | 0.1463 mL | 0.7316 mL | 1.4632 mL | 3.6579 mL | |
| 20 mM | 0.1097 mL | 0.5487 mL | 1.0974 mL | 2.7435 mL | |
| 25 mM | 0.0878 mL | 0.4390 mL | 0.8779 mL | 2.1948 mL | |
| 30 mM | 0.0732 mL | 0.3658 mL | 0.7316 mL | 1.8290 mL | |
| 40 mM | 0.0549 mL | 0.2743 mL | 0.5487 mL | 1.3717 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0974 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.9145 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2743 mL | 0.6859 mL | |
| 100 mM | 0.0219 mL | 0.1097 mL | 0.2195 mL | 0.5487 mL |
Cadisegliatin Related Classifications
HY-147254 Related Classifications
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