CD38-IN-6
CD38-IN-6 is an orally active CD38 inhibitor. CD38-IN-6 regulates NAD+ metabolite levels in the liver of aged obese mice by increasing NAD+ and NMN levels, and decreasing NAM and ADPR levels. CD38-IN-6 alleviates inflammatory responses in mice. CD38-IN-6 can be used for research related to obesity and inflammation.
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- Pureza: 99.96%
- No. CAS: 2766686-04-6
- Fòrmula: C17H15F3N6O3
- Peso molecular:408.33
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
CD38-IN-6 (Compound 39) (8 different concentrations; 10 min) potently inhibits 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 regulates intracellular calcium flux in CD38-expressing NH7-dCas9 Jurkat T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CD38-IN-6 (10 mg/kg; p.o.; twice daily; for 5 consecutive days) regulates 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; p.o.) alleviates LPS (HY-D1056)-induced inflammatory responses in mice by reducing proinflammatory cytokines, regulating NAD+ metabolite levels in the spleen and liver, and decreasing CD38 expression and inflammatory gene expression in the liver[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL6/J (male, 7.5 months old, diet-induced obese)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:p.o.; single dose/p.o.; twice daily; 49 days
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Result:Increased liver NAD+ and NMN levels relative to vehicle control.
Decreased liver NAM and ADPR levels relative to vehicle control.
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Animal Model:C57BL6/J (male, 19-22 months old, diet-induced obese)[1]
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Dosage:10 mg/kg
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Administration:p.o.; twice daily; 5 days
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Result:Increased liver NAD+ and NMN levels relative to vehicle control.
Decreased liver NAM and ADPR levels relative to vehicle control.
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Animal Model:C57BL/6J (male, 12 weeks old, LPS-induced inflammation)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.
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Result:Caused statistically significant decreases in plasma IL-6, TNFα, and IP-10 at 8-hour post-LPS challenge.
Caused statistically significant decreases in plasma IP-10 at 4-hour post-LPS challenge; 10 mg/kg caused a 43% decrease in IL-6 and 22% decrease in TNFα; 30 mg/kg caused a 75% decrease in IL-6 and 58% decrease in TNFα.
Caused a 2.3-fold increase in spleen NAD+ levels and a 40% decrease in spleen ADPR levels at 8-hour post-LPS challenge; 10 mg/kg and 30 mg/kg caused statistically significant decreases in spleen MIP1α, MIP2, TNFα, RANTES, MCP1, IL-1β, IL-6, IP-10, and IFNγ levels at 8-hour post-LPS challenge.
Caused a 2-fold increase in liver NAD+ levels at 8-hour post-LPS challenge, and 30 mg/kg caused a 38% decrease in liver NAM levels at 8-hour post-LPS challenge; caused decreases in liver ADPR levels at 4-hour post-LPS challenge; caused statistically significant decreases in liver CD38 expression, as well as statistically significant decreases in liver MIP1α, MIP2, TNFα, RANTES, MCP1, IL-1β, IL-6, IP-10, and IFNγ levels at 8-hour post-LPS challenge.
Chemical Information
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No. CAS 2766686-04-6
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Appearance Solid
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Peso molecular 408.33
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Fòrmula C17H15F3N6O3
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Color White to off-white
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 27 mg/mL (66.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.7 mg/mL (6.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.7 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.7 mg/mL (6.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.7 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4490 mL | 12.2450 mL | 24.4900 mL | 61.2250 mL |
| 5 mM | 0.4898 mL | 2.4490 mL | 4.8980 mL | 12.2450 mL | |
| 10 mM | 0.2449 mL | 1.2245 mL | 2.4490 mL | 6.1225 mL | |
| 15 mM | 0.1633 mL | 0.8163 mL | 1.6327 mL | 4.0817 mL | |
| 20 mM | 0.1224 mL | 0.6122 mL | 1.2245 mL | 3.0612 mL | |
| 25 mM | 0.0980 mL | 0.4898 mL | 0.9796 mL | 2.4490 mL | |
| 30 mM | 0.0816 mL | 0.4082 mL | 0.8163 mL | 2.0408 mL | |
| 40 mM | 0.0612 mL | 0.3061 mL | 0.6122 mL | 1.5306 mL | |
| 50 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2245 mL | |
| 60 mM | 0.0408 mL | 0.2041 mL | 0.4082 mL | 1.0204 mL |
CD38-IN-6 Related Classifications
HY-186178 Related Classifications
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