Art. -Nr.: HY-13070

MK-8245

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

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.

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Reinheit: 99.04%
CAS. Nr.: 1030612-90-8
Formel: C₁₇H₁₆BrFN₆O₄
Molecular Weight:467.25

Speicherung:

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)

MK-8245 Chemical Structure

CAS. Nr.: 1030612-90-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	IC₅₀	5 nM Compound: 7, MK-8245	Inhibition of SCD-1 activity in human Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation after 1 hr by scintillation counting Inhibition of SCD-1 activity in human Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation after 1 hr by scintillation counting	[PMID: 21661758]
Hepatocyte	IC₅₀	68 nM Compound: 7, MK-8245	Inhibition of SCD-1 activity in Sprague-Dawley rat Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting Inhibition of SCD-1 activity in Sprague-Dawley rat Hepatocytes expressing organic anion transporting polypeptides assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting	[PMID: 21661758]
Hepatocyte	IC₅₀	68 nM Compound: MK-8245	Inhibition of SCD1 in rat hepatocytes expressing OATP Inhibition of SCD1 in rat hepatocytes expressing OATP	[PMID: 22101133]
HepG2	IC₅₀	>100000 μM Compound: 7, MK-8245	Inhibition of human delta6 desaturase activity expressed in human HEpG2 cells Inhibition of human delta6 desaturase activity expressed in human HEpG2 cells	[PMID: 21661758]
HepG2	IC₅₀	>100000 μM Compound: 7, MK-8245	Inhibition of rat delta-5 desaturase activity expressed in human HEpG2 cells Inhibition of rat delta-5 desaturase activity expressed in human HEpG2 cells	[PMID: 21661758]
HepG2	IC₅₀	>100000 μM Compound: 7, MK-8245	Inhibition of rat delta-6 desaturase activity expressed in human HEpG2 cells Inhibition of rat delta-6 desaturase activity expressed in human HEpG2 cells	[PMID: 21661758]
HepG2	IC₅₀	1066 nM Compound: 7, MK-8245	Inhibition of SCD-1 activity in organic anion transporting polypeptides-deficient human HepG2 cells assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting Inhibition of SCD-1 activity in organic anion transporting polypeptides-deficient human HepG2 cells assessed as reduction in [I-14C] stearoyl CoA desaturation by scintillation counting	[PMID: 21661758]
HepG2	IC₅₀	>100000 μM Compound: 7, MK-8245	Inhibition of human delta-5 desaturase activity expressed in human HEpG2 cells Inhibition of human delta-5 desaturase activity expressed in human HEpG2 cells	[PMID: 21661758]
HepG2	IC₅₀	1070 nM Compound: MK-8245	Inhibition of SCD1 in OATP-deficient human HepG2 cells by whole cell assay Inhibition of SCD1 in OATP-deficient human HepG2 cells by whole cell assay	[PMID: 22101133]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1030612-90-8
Appearance Solid
Molecular Weight 467.25
Formel C₁₇H₁₆BrFN₆O₄
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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 (4)

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Journal Impact Factor

Sci China Life Sci

NPC1-regulated dynamic of clathrin-coated pits is essential for viral entry. [Abstract]

2022 Feb;65(2):341-361. PMID: 34047913
Elife

Amelioration of non-alcoholic fatty liver disease by targeting adhesion G protein-coupled receptor F1 ( Adgrf1). [Abstract]

2023 Aug 15:12:e85131. PMID: 37580962
Neurosci Bull

Targeting Phospholipid Metabolism as an Effective Hearing Protection Strategy. [Abstract]

2025 Jun 28. PMID: 40580390
Aquaculture

2023 Jun 10, 739766.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1402 mL

10.7009 mL

21.4018 mL

5 mM

0.4280 mL

2.1402 mL

4.2804 mL

10 mM

0.2140 mL

1.0701 mL

2.1402 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (596 KB)
- English - EN (596 KB)
- Français - FR (596 KB)
- Deutsch - DE (596 KB)
- Norwegian - NO (596 KB)
- Español - ES (596 KB)
- Swedish - SV (596 KB)
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- Portuguese - PT (596 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Oballa RM, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MK-8245

4 Cited Publications

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MK-8245

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Publications Citing Use of MedChemExpress (MCE) MK-8245

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MK-8245

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-COVID-19 Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MK-8245

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MK-8245 Related Classifications

HY-13070 Related Classifications