| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Nampt-IN-17 (N16) (concentration variable; 30 min) potently inhibits recombinant human NAMPT enzyme via a non-competitive mechanism, with an IC50 value of 17 nM. It exhibits much higher selectivity for NAMPT than HDAC and most kinases, and moderate inhibitory activity against certain CYP450 isoenzymes (especially CYP3A4/5) [1]. Nampt-IN-17 (3.1–100 μM) can directly bind to recombinant human NAMPT, with a Kd value of 9.17 μM [1]. Nampt-IN-17 (72 h) selectively and potently inhibits the activity of NAPRT-deficient gastric cancer cells (HGC-27, MKN-74, MKN-45), with an IC50 value ranging from 0.0013 to 0.017 μM, while having no effect on normal cells and cancer cells expressing NAPRT [1]. Nampt-IN-17 (0.1-60 nM; 24-48 hours) effectively and dose-dependently inhibited the proliferation and colony formation of NAPRT-deficient HGC-27 and MKN-74 gastric cancer cells [1]. Nampt-IN-17 (0.1-1.6 nM; 24 hours) dose-dependently inhibited the migration and invasion of NAPRT-deficient HGC-27 gastric cancer cells [1]. Nampt-IN-17 (1.6-6.4 nM; 48 hours) dose-dependently induced S-phase and G2/M-phase cell cycle arrest and apoptosis in NAPRT-deficient HGC-27 gastric cancer cells [1]. Nampt-IN-17 (1.6-6.4 nM; 24-48 hours) dose-dependently depletes intracellular NAD+ and ATP levels and disrupts the mitochondrial membrane potential of NAPRT-deficient HGC-27 gastric cancer cells. Its effects can be reversed by NMN but not by niacin [1].
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| ln Vivo |
N16 (7.5–15 mg/kg; gavage; twice daily; 12 days) showed dose-dependent in vivo antitumor efficacy against NAPRT-deficient HGC-27 gastric cancer xenografts, with a maximum TGI of 78.9% at 15 mg/kg twice daily [1].
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (male; 4-5 weeks old for efficacy studies; 6 weeks old for short-term toxicity studies; subcutaneous transplantation of NAPRT-deficient HGC-27 cells) [1]
Doses: 7.5 mg/kg Route of Administration: Gavage; twice daily; 12 days Experimental Results: Tumor growth inhibition rate (TGI) reached 65.3%, and the final tumor weight was reduced compared with the vector without causing significant weight loss or organ toxicity (no histological abnormalities were observed in the heart, liver, lungs, spleen or kidneys). Animal/Disease Models:BALB/c nude mice (male; 4-5 weeks old for efficacy studies; 6 weeks old for short-term toxicity studies; subcutaneous transplantation of NAPRT-deficient HGC-27 cells) [1] Doses: 15 mg/kg Route of Administration: Gavage; twice daily; 12 days Experimental Results: Tumor growth inhibition rate reached 78.9%, and the final tumor weight was reduced compared with the vector, but from day 5 onwards, it led to a gradual decrease in body weight and the appearance of spleen histological abnormalities (reduced nuclei of blue-purple stained cells, indicating lymphocyte depletion). |
| References |
| Molecular Formula |
C26H28FN5O2
|
|---|---|
| Molecular Weight |
461.53
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| CAS # |
3077970-78-3
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC1=CC=C(C(C(N[C@H](C2=CC=C(C=C2)NC(NCC3=CC=CN=C3)=O)C)=O)=C1)N4CCCC4
|
| 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)
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| 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 | 2.1667 mL | 10.8335 mL | 21.6671 mL | |
| 5 mM | 0.4333 mL | 2.1667 mL | 4.3334 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1667 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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