| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
NAMPT activator-10 (0-8.0 μM) can effectively activate purified NAMPT enzyme in a concentration-dependent manner, with a maximum activation rate of 206%[1]. NAMPT activator-10 (0-5.00 μM) has a high affinity for purified NAMPT enzyme (Kd = 0.64 μM)[1]. NAMPT activator-10 (0-4.0 μM; 4 h) can increase NAD+ levels in THLE-2 hepatocytes in a concentration-dependent manner over 4 hours[1]. NAMPT activator-10 (72 h) showed low cytotoxicity after 72 hours of treatment in THLE-2 hepatocytes (IC50 = 316 μM) and C2C12 mouse myotube cells (IC50 = 236 μM)[1]. NAMPT activator-10 (1.25–10.0 μM) increases the phosphorylation level of AMPK in the myotubules of C2C12 mice in a concentration-dependent manner [1].
|
|---|---|
| ln Vivo |
Compound B11 (20 mg/kg; intraperitoneal injection; daily; 3 days) relieves muscle fatigue by reducing lactate buildup and increasing energy reserves in the liver and muscle tissue [1].
|
| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 7 weeks old, 19-23 g, muscle fatigue model established by running on a treadmill for 1 hour daily for 6 consecutive days) [1]
Doses: 20 mg/kg Route of Administration: Intraperitoneal injection; once daily for 3 consecutive days Experimental Results: Serum lactate level was significantly reduced. Serum lactate dehydrogenase content was increased. Liver glycogen reserves increased by 3.1 times compared to the control group. Muscle glycogen reserves increased by 1.5 times compared to the control group. Animal/Disease Models:C57BL/6J (male, 7 weeks old, 19-23 g, treadmill exercise-induced muscle fatigue injury model) [1] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection; once daily for 3 consecutive days Experimental Results: Compared with the fatigue model group, the experimental group maintained the integrity of skeletal muscle ultrastructure, orderly arrangement of myofibrils, reduced sarcoplasmic vacuolation, increased mitochondrial volume and number, and intact mitochondrial cristae. Skeletal muscle NAD+ level increased by 1.5 times compared with the control group. Skeletal muscle ATP level increased by 1.8 times compared with the control group. NAD+ and ATP levels in heart, liver and kidney tissues were significantly increased. No pathological abnormalities were found in major organs. |
| References |
| Molecular Formula |
C20H20N4O4S
|
|---|---|
| Molecular Weight |
412.46
|
| CAS # |
2237269-22-4
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC1=CC=C(C=C1)NS(=O)(C2=CC=C(C=C2)OC)=O)NCC3=CC=NC=C3
|
| 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 | 2.4245 mL | 12.1224 mL | 24.2448 mL | |
| 5 mM | 0.4849 mL | 2.4245 mL | 4.8490 mL | |
| 10 mM | 0.2424 mL | 1.2122 mL | 2.4245 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
