2. Immunology/Inflammation
  3. CD38
  4. MK-0159

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.

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MK-0159 Chemical Structure

MK-0159 Chemical Structure

CAS No. : 2641484-61-7

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Based on 1 publication(s) in Google Scholar

MK-0159 Related Antibodies

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  • Purity & Documentation

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Description

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[1].

IC50 & Target

IC50: 3 nM (mouse CD38), 22 ± 5 nM (hCD38), 70 nM (rat CD38)[1]
In Vitro

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 Related Antibodies
In Vivo

MK-0159 (3-30 mg/kg, p.o., a single dose) increases systemic NAD+ and decreases ADPR levels (the product and substrate of CD38 enzymatic activity) in blood and heart of mice[1].
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.

Animal Model: Cardiac I/R injury mice[1]
Dosage: 30 mg/kg
Administration: p.o.
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.
Molecular Weight

400.49

Formula

C20H24N4O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C(NC=C2)=NC(C3=CN=CS3)=C1)N[C@H]4CC[C@H](OCCOC)CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4969 mL 12.4847 mL 24.9694 mL
5 mM 0.4994 mL 2.4969 mL 4.9939 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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MK-0159 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-01592641484-61-7MK0159MK 0159CD38NAD+NADP+ADPRorally activeCardiovascular diseasemetabolic diseasesInhibitorinhibitorinhibit

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