MK-8245
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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- Purity: 99.04%
- CAS No.: 1030612-90-8
- 화학식: C17H16BrFN6O4
- 분자량:467.25
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보관:
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)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MK-8245
More
Biological Activity
IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SCD1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
5 nM
Compound: 7, MK-8245
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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
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[PMID: 21661758] |
| Hepatocyte | IC50 |
68 nM
Compound: 7, MK-8245
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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
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[PMID: 21661758] |
| Hepatocyte | IC50 |
68 nM
Compound: MK-8245
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Inhibition of SCD1 in rat hepatocytes expressing OATP
Inhibition of SCD1 in rat hepatocytes expressing OATP
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[PMID: 22101133] |
| HepG2 | IC50 |
>100000 μM
Compound: 7, MK-8245
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Inhibition of human delta6 desaturase activity expressed in human HEpG2 cells
Inhibition of human delta6 desaturase activity expressed in human HEpG2 cells
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[PMID: 21661758] |
| HepG2 | IC50 |
>100000 μM
Compound: 7, MK-8245
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Inhibition of rat delta-5 desaturase activity expressed in human HEpG2 cells
Inhibition of rat delta-5 desaturase activity expressed in human HEpG2 cells
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[PMID: 21661758] |
| HepG2 | IC50 |
>100000 μM
Compound: 7, MK-8245
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Inhibition of rat delta-6 desaturase activity expressed in human HEpG2 cells
Inhibition of rat delta-6 desaturase activity expressed in human HEpG2 cells
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[PMID: 21661758] |
| HepG2 | IC50 |
1066 nM
Compound: 7, MK-8245
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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
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[PMID: 21661758] |
| HepG2 | IC50 |
>100000 μM
Compound: 7, MK-8245
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Inhibition of human delta-5 desaturase activity expressed in human HEpG2 cells
Inhibition of human delta-5 desaturase activity expressed in human HEpG2 cells
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[PMID: 21661758] |
| HepG2 | IC50 |
1070 nM
Compound: MK-8245
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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
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[PMID: 22101133] |
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.
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.
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Animal Model:Male C57BL6 mice, male Sprague-Dawley rats[1]
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Dosage:10mg/kg
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Administration:Oral administration
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Result:Exhibits a tissue distribution profile concentrated in the liver.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1030612-90-8
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Appearance Solid
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분자량 467.25
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화학식 C17H16BrFN6O4
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Color White to off-white
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SMILES
O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
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Most Recent
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Sci China Life Sci
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
2025 Jun 28. PMID: 40580390 -
용액&용해도
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.
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.
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: ≥ 2.5 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.
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.
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.
순도&문서
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Data Sheet (273 KB)
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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)
- Italian - IT (596 KB)
- Korean - KR (596 KB)
- Portuguese - PT (596 KB)
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Handling Instructions (2659 KB)
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 | 2.1402 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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