| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CD38-IN-6 (compound 39) (8 different concentrations; 10 min) effectively inhibited CD38-mediated NAD+ hydrolase activity in primary human M1 macrophages, with an IC50 of 3.9 nM [1]. CD38-IN-6 (50 nM; 24 h) significantly regulated intracellular calcium ion flow in CD38-expressing NH7-dCas9 Jurkat T cells [1].
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| ln Vivo |
CD38-IN-6 (1-10 mg/kg; orally; once or twice daily; for 49 days) modulates NAD+ metabolite levels in the liver of obese mice by increasing NAD+ and NMN levels and decreasing NAM and ADPR levels [1]. CD38-IN-6 (10 mg/kg; orally; twice daily; for 5 days) modulates NAD+ metabolite levels in the liver of aged obese mice by increasing NAD+ and NMN levels and decreasing NAM and ADPR levels [1]. CD38-IN-6 (10-30 mg/kg; orally) modulates NAD+ metabolite levels in the spleen and liver by reducing pro-inflammatory cytokines and reducing CD38 expression and inflammatory gene expression in the liver, thereby alleviating LPS-induced inflammatory responses in mice [1].
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| Animal Protocol |
Animal/Disease Models:C57BL6/J (male, 7.5 months old, diet-induced obesity) [1]
Doses: 1 mg/kg; 10 mg/kg Route of Administration: Oral; Single oral dose; Twice daily; 49 days Experimental Results: Liver NAD+ and NMN levels were increased compared to the solvent control group. Liver NAM and ADPR levels were decreased compared to the solvent control group. Animal/Disease Models:C57BL6/J (male, 19-22 months old, diet-induced obesity) [1] Doses: 10 mg/kg Route of Administration: Oral; twice daily; 5 days Experimental Results: Liver NAD+ and NMN levels were increased compared to the solvent control group. Liver NAM and ADPR levels were decreased compared to the solvent control group. Animal/Disease Models:C57BL/6J (male, 12 weeks old, LPS-induced inflammation) [1] Doses: 10 mg/kg; 30 mg/kg Route of Administration: Oral Experimental Results: 8 hours after LPS stimulation, plasma IL-6, TNFα and IP-10 levels were significantly reduced. 4 hours after LPS stimulation, plasma IP-10 levels were significantly reduced; in the 10 mg/kg dose group, IL-6 levels decreased by 43% and TNFα levels decreased by 22%; in the 30 mg/kg dose group, IL-6 levels decreased by 75% and TNFα levels decreased by 58%. Eight hours after LPS stimulation, spleen NAD+ levels increased 2.3-fold, and spleen ADPR levels decreased by 40%. In both the 10 mg/kg and 30 mg/kg groups, spleen MIP1α, MIP2, TNFα, RANTES, MCP1, IL-1β, IL-6, IP-10, and IFNγ levels were significantly decreased eight hours after LPS stimulation. Eight hours after LPS stimulation, liver NAD+ levels increased 2-fold, and in the 30 mg/kg group, liver NAM levels decreased by 38% eight hours after LPS stimulation; liver ADPR levels decreased four hours after LPS stimulation. Eight hours after LPS stimulation, liver CD38 expression showed a statistically significant decrease, as did liver MIP1α, MIP2, TNFα, RANTES, MCP1, IL-1β, IL-6, IP-10, and IFNγ levels. |
| References |
| Molecular Formula |
C17H15F3N6O3
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|---|---|
| Molecular Weight |
408.33
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| CAS # |
2766686-04-6
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C1=NC(N2C=NC=C2)=NC(OCCOC)=C1)NC3=CC(C(F)(F)F)=NC=C3
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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)
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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 | 2.4490 mL | 12.2450 mL | 24.4900 mL | |
| 5 mM | 0.4898 mL | 2.4490 mL | 4.8980 mL | |
| 10 mM | 0.2449 mL | 1.2245 mL | 2.4490 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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