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

MK-8245 

Cat. No.: HY-13070 Purity: 99.82%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 123 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
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50 mg USD 540 In-stock
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100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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].

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.
Molecular Weight

467.25

Formula

C₁₇H₁₆BrFN₆O₄

CAS No.

1030612-90-8

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 : 19 mg/mL (40.66 mM; Need ultrasonic and warming)

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
10 mM 0.2140 mL 1.0701 mL 2.1402 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.82%

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MK-8245
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HY-13070
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