MK-8245

Alias: MK-8245; MK 8245; MK8245; 4-(2-Bromo-5-fluorophenoxy)-1-[5-(2H-tetrazol-5-yl)-3-isoxazolyl]piperidine
Cat No.:V0856 Purity: ≥98%
MK-8245 (MK8245; MK 8245) is a novel and potentliver-targeted inhibitor of stearoyl-CoA desaturase (SCD) with anti-diabetic and anti-dyslipidemic activities.
MK-8245 Chemical Structure CAS No.: 1030612-90-8
Product category: Dehydrogenase
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of MK-8245:

  • MK-8245 Trifluoroacetate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

MK-8245 (MK8245; MK 8245) is a novel and potent liver-targeted inhibitor of stearoyl-CoA desaturase (SCD) with anti-diabetic and anti-dyslipidemic activities. It inhibits stearoyl-CoA desaturase with an IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. It exhibits high anti-diabetic and anti-dyslipidemic efficacy in vivo and a significantly improved therapeutic window.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
MK-8245 is an effective SCD inhibitor that is liver-specific[1]. With IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1, MK-8245 has comparable potencies against SCD1 in humans, rats, and mice[1]. In the rat hepatocyte assay, where organic anion transporting polypeptides (OATPs) are functional and active with an IC50 of 68 nM, MK-8245 shows a considerable reduction of SCD. In the HepG2 cell assay, on the other hand, OATPs are only weakly active and have an IC50 of approximately 1 μM, indicating a lack of activity[1].
ln Vivo
In rats, dogs, and rhesus monkeys, MK-8245 (10 mg/kg; po) has a tissue distribution profile that is concentrated in the liver and has little exposure in tissues linked to possible adverse events[1]. When given to eDIO mice before to the glucose challenge, MK-8245 increases glucose clearance in a dose-dependent manner[1].
Animal Protocol
Animal/Disease Models: Male C57BL6 mice, male SD (Sprague-Dawley) rats[1]
Doses: 10mg/kg
Route of Administration: Oral administration
Experimental Results: Exhibits a tissue distribution profile concentrated in the liver.
References
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H16N6O4FBR
Molecular Weight
467.24914
CAS #
1030612-90-8
SMILES
FC1=CC=C(Br)C(OC2CCN(C3=NOC(C4=NNN=N4)=C3)CC2)=C1
InChi Key
UDXUBDGJHLPKFJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H14BrFN6O2/c16-11-2-1-9(17)7-12(11)24-10-3-5-23(6-4-10)14-8-13(25-20-14)15-18-21-22-19-15/h1-2,7-8,10H,3-6H2,(H,18,19,21,22)
Synonyms
MK-8245; MK 8245; MK8245; 4-(2-Bromo-5-fluorophenoxy)-1-[5-(2H-tetrazol-5-yl)-3-isoxazolyl]piperidine
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 93 mg/mL (199.0 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
1% CMC+0.5% Tween-80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.2140 mL 1.0701 mL 2.1402 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
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