| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Teglicar (0-3 mM; 1 min) chloride potently and selectively inhibits the liver isoenzyme CPT I (L-CPT I) in rat liver mitochondria with an IC50 of 1.1 μM, while its inhibitory efficacy against the heart isoenzyme CPT I (M-CPT I) in rat heart mitochondria is 39.4 times lower with an IC50 of 43.4 μM [1]. Teglicar (up to 50 μM; 48 h) chloride showed no cytotoxicity to rat hepatocytes after incubation at concentrations up to 50 μM for 48 hours [1]. Teglicar (0.5-1.0 μM) chloride exhibited reversible mixed inhibitory effects on L-CPT I expressed by Pichia pastoris, and its inhibitory effect on palmitoyl-CoA was shown by an apparent Ki value of 0.36 ± 0.04 μM [1].
|
|---|---|
| ln Vivo |
Ticagliflozin chloride (50 mg/kg; orally; twice daily; 45 days) reduced serum glucose levels in male C57BL/KsJ-db/db mice by 25% and improved glucose homeostasis without affecting cardiac parameters [1]. Ticagliflozin chloride (10-40 mg/kg; orally) reduced serum β-hydroxybutyrate levels in male Sprague Dawley rats that had been fasted for 24 hours in a dose-dependent manner, with an ED50 of 14.5 mg/kg [1].
|
| Animal Protocol |
Animal/Disease Models:C57BL/KsJ-db/db (male, 8 weeks old) [1]
Doses: 50 mg/kg Route of Administration: Oral; twice daily for 45 days Experimental Results: Serum glucose levels decreased by 25% (from 673.9 ± 44.09 mg/dL to 506.6 ± 59.12 mg/dL). Serum fructosamine levels decreased by 30% (from 4.80 ± 0.17 mmol/L to 3.36 ± 0.30 mmol/L). Liver glycogen content decreased by 25%. Liver triglyceride content increased by 38%. Serum free fatty acid levels increased by 20%. No significant changes were observed in serum insulin, leptin, triglycerides, urea, alanine aminotransferase, or cholesterol levels. No effect was observed on heart weight or cardiac triglyceride content. |
| References |
| Molecular Formula |
C22H46CLN3O3
|
|---|---|
| Molecular Weight |
436.07
|
| CAS # |
908566-80-3
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CCCCCCCCCCCCCCNC(N[C@H](CC(O)=O)C[N+](C)(C)C)=O.[Cl-]
|
| Synonyms |
ST1326 chloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.2932 mL | 11.4660 mL | 22.9321 mL | |
| 5 mM | 0.4586 mL | 2.2932 mL | 4.5864 mL | |
| 10 mM | 0.2293 mL | 1.1466 mL | 2.2932 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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