| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
LCZ960 (0-300 mg/kg, oral, once daily, 14-18 days) increased liver glycogen excess and antibody tolerance and reduced blood pressure in a diet-induced exercise (DIO) model [1]. LCZ960 (0-30 mg/kg, oral, once daily, 7 days) reduced and improved blood glucose levels in a DIO model [1]. LCZ960 (60 mg/kg, liver, once daily) increased liver glycogen storage, glycogen synthesis (Vsyn), glycogenolysis, liver glycogen turnover, and glycogen curve variables in a SD model, and inhibited curve concentration variables [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models: DIO mice (male C57Bl/6, 23-32 g) model[1]
Doses: 30 mg/kg Route of Administration: p.o. once/once a day, 18 days Experimental Results: Increased the liver over plasma levels. Animal/Disease Models: DIO mice (male C57Bl/6, 23-32 g) model[1] Doses: 0, 10, 30, 100 and 300 mg/kg Route of Administration: p.o., once/once a day, 2 weeks Experimental Results: Showed dose-dependent blood glucose reduction over 24 h without reaching the hypoglycemic state, even at a very high dose of 300 mg/kg, did not lower fasting blood glucose into the hypoglycemic range. Dose-dependent improved glucose tolerance at 2 weeks, decreased insulin AUC at 100 mg/kg. Animal/Disease Models: DIO rat (male SD, 480 g) model[1] Doses: 0, 10, 30 mg/kg Route of Administration: p.o., once a day, 7 days Experimental Results: Decreased blood glucose levels and improved glucose excursion (significant at 30 mg/kg) at day 7. Animal/Disease Models: SD rat (male SD, 480 g) model[1] Doses: 60 mg/kg Route of Administration: p.o., once Experimental Results: Did not further increase glucose-stimulated G6P accumulation but clearly augmented hepatic glycogen storage during the first 2 h of infusion. Increased the true rate of glycogen synthesis (Vsyn), glycogen breakdown, hepatic glycogen turnover, hepatic glycogen concentrations, plasma glucose concentrations, suppressed plasma lactate concentrations. |
| References |
| Molecular Formula |
C30H34N6O3S2
|
|---|---|
| Molecular Weight |
590.76
|
| CAS # |
1067877-83-1
|
| Appearance |
Typically exists as solids at room temperature
|
| Synonyms |
NVP-LCZ960
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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)
|
| 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 | 1.6927 mL | 8.4637 mL | 16.9273 mL | |
| 5 mM | 0.3385 mL | 1.6927 mL | 3.3855 mL | |
| 10 mM | 0.1693 mL | 0.8464 mL | 1.6927 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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