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

MK-8245 

Cat. No.: HY-13070 Purity: 99.33%
Handling Instructions

MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.

For research use only. We do not sell to patients.
MK-8245 Chemical Structure

MK-8245 Chemical Structure

CAS No. : 1030612-90-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 185 In-stock
2 mg USD 120 In-stock
5 mg USD 180 In-stock
10 mg USD 288 In-stock
50 mg USD 888 In-stock
100 mg USD 1320 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

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Description

MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) [1] Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. 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. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1]. in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg.

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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.
References
Molecular Weight

467.25

Formula

C₁₇H₁₆BrFN₆O₄

CAS No.

1030612-90-8

Storage

4°C, protect from light

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 19 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.33%

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Product Name:
MK-8245
Cat. No.:
HY-13070
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