1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)
  3. MK-8245

MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy.

For research use only. We do not sell to patients.

MK-8245 Chemical Structure

MK-8245 Chemical Structure

CAS No. : 1030612-90-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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USD 123 In-stock
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10 mM * 1 mL in DMSO USD 123 In-stock
Solid
2 mg USD 60 In-stock
5 mg USD 120 In-stock
10 mg USD 190 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of MK-8245:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy[1].

IC50 & Target

IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SCD1)[1]

In Vitro

MK-8245 is a potent and liver-specific SCD inhibitor[1].
MK-8245 displays similar potencies against human, rat and mouse SCD1, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1[1].
MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, actives organic anion transporting polypeptides (OATPs) with IC50 of 68 nM, while being only weakly active OATPs in the HepG2 cell assay which is devoid of active with IC50 of ~1 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MK-8245 (10mg/kg; p.o.) exhibits a tissue distribution profile concentrated in the liver, with low exposure in tissues associated with potential adverse events in rats, dogs, and rhesus monkeys[1].
MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before the glucose challenge[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL6 mice, male Sprague-Dawley rats[1]
Dosage: 10mg/kg
Administration: Oral administration
Result: Exhibits a tissue distribution profile concentrated in the liver.
Clinical Trial
Molecular Weight

467.25

Formula

C17H16BrFN6O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (214.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1402 mL 10.7009 mL 21.4018 mL
5 mM 0.4280 mL 2.1402 mL 4.2804 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 (protect from 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
×
Volume
×
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

×
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 (5.35 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 (5.35 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 (protect from 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

Purity: 98.99%

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 (protect from 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 2.1402 mL 10.7009 mL 21.4018 mL 53.5045 mL
5 mM 0.4280 mL 2.1402 mL 4.2804 mL 10.7009 mL
10 mM 0.2140 mL 1.0701 mL 2.1402 mL 5.3505 mL
15 mM 0.1427 mL 0.7134 mL 1.4268 mL 3.5670 mL
20 mM 0.1070 mL 0.5350 mL 1.0701 mL 2.6752 mL
25 mM 0.0856 mL 0.4280 mL 0.8561 mL 2.1402 mL
30 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7835 mL
40 mM 0.0535 mL 0.2675 mL 0.5350 mL 1.3376 mL
50 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0701 mL
60 mM 0.0357 mL 0.1783 mL 0.3567 mL 0.8917 mL
80 mM 0.0268 mL 0.1338 mL 0.2675 mL 0.6688 mL
100 mM 0.0214 mL 0.1070 mL 0.2140 mL 0.5350 mL
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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.

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MK-8245
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