MK-0159
Based on 1 publication(s) in Google Scholar
MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD+ (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.60%
- CAS 番号: 2641484-61-7
- 分子式: C20H24N4O3S
- 分子量:400.49
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 MK-0159
More
生物活性
IC50: 3 nM (mouse CD38), 22 ± 5 nM (hCD38), 70 nM (rat CD38)[1]
MK-0159 (compound 37) (0-50 μM, 24 h) increases both extracellular and intracellular NAD+ in A549 cells and HMVEC cells[1].
MK-0159 (20 μM, overnight) reduces the number of cells with damaged mitochondria in CD38-overexpressing CD8+ T cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MK-0159 (30 mg/kg, p.o.) reduces infarct size in cardiac I/R injury mice[2].
MK-0159 (30 mg/kg, oral gavage, twice a day for 9 days) reverses mitochondrial defect, restores CD8+ T cell function and inhibits virally induced organ inflammation in BXD2 lupus-prone mice with LCMV infection[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cardiac I/R injury mice[1]
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Dosage:30 mg/kg
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Administration:p.o.
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Result:Reduced infarct size, and the combination of MK-0159 and NAD+ precursor significantly reduced the infarct size compared to MK-0159 alone.
Increased whole heart NAD+ levels and decreased ADPR in the heart.
化学情報
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CAS 番号 2641484-61-7
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性状 Solid
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分子量 400.49
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分子式 C20H24N4O3S
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Color White to off-white
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SMILES
O=C(C1=C2C(NC=C2)=NC(C3=CN=CS3)=C1)N[C@H]4CC[C@H](OCCOC)CC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
CD38-Targeted Small-Molecule PET Radiotracer for Noninvasive Tumor Evaluation and Preliminary Therapy Monitoring in Multiple Myeloma. [Abstract]2026 Mar 26;69(6):7068-7081. PMID: 41837524
溶剤 & 溶解度
DMSO : 100 mg/mL (249.69 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 and light). 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.5 mg/mL (6.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 and light)
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.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
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- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Lagu B, et al. Orally Bioavailable Enzymatic Inhibitor of CD38, MK-0159, Protects against Ischemia/Reperfusion Injury in the Murine Heart. J Med Chem. 2022 Jun 28. [Content Brief]
[2]. Chen PM, et al. CD38 reduces mitochondrial fitness and cytotoxic T cell response against viral infection in lupus patients by suppressing mitophagy. Sci Adv. 2022 Jun 17;8(24):eabo4271. [Content Brief]
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 and light). 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 | 2.4969 mL | 12.4847 mL | 24.9694 mL | 62.4235 mL |
| 5 mM | 0.4994 mL | 2.4969 mL | 4.9939 mL | 12.4847 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4969 mL | 6.2424 mL | |
| 15 mM | 0.1665 mL | 0.8323 mL | 1.6646 mL | 4.1616 mL | |
| 20 mM | 0.1248 mL | 0.6242 mL | 1.2485 mL | 3.1212 mL | |
| 25 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4969 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8323 mL | 2.0808 mL | |
| 40 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5606 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0404 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 mL | |
| 100 mM | 0.0250 mL | 0.1248 mL | 0.2497 mL | 0.6242 mL |
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