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MK-8245

Catalog No. T2650 CAS 1030612-90-8

MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function.

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MK-8245, CAS 1030612-90-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 287.00
50 mg	In stock	$ 492.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99%

Purity: 98.77%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function.
Targets&IC50	SCD1 (rat):3 nM, SCD1 (human):1 nM, SCD1 (mouse):3 nM
In vitro	In mice, rats, dogs, and cynomolgus monkeys, the primary site of action for MK-8245 (p.o.) is the liver, displaying minimal efficacy in tissues associated with potential adverse reactions. In eDIO mice, MK-8245 demonstrates a dose-dependent effect on glucose screening, enhancing glucose clearance (ED50: 7 mg/kg).
In vivo	In experiments conducted on rat liver cells exhibiting functional activity of OATPs, MK-8245 demonstrated a potent inhibitory effect on SCD, with an IC50 of 68 nM. However, in experiments with HepG2 cells, which lack active OATPs, the compound was less effective, showing an IC50 of 1 μM. In HepG experiments, MK-8245 displayed high selectivity towards Δ-5 and Δ-6 desaturases. MK-8245 contains a tetrazole acetic acid group, endowing it with the capability for OATP recognition and liver-targeting functions.
Kinase Assay	High Throughput Screening: FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program.

Molecular Weight	467.25
Formula	C17H16BrFN6O4
CAS No.	1030612-90-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 86 mg/mL (184.1 mM)

References and Literature

1. Oballa RM, et al. J Med Chem, 2011, 54(14), 5082-5096.

Related compound libraries

This product is contained In the following compound libraries：

Fluorochemical Library Clinical Compound Library Drug Repurposing Compound Library NO PAINS Compound Library Inhibitor Library ReFRAME Related Library Anti-Obesity Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MK-8245 1030612-90-8 Metabolism Dehydrogenase Stearoyl-CoA Desaturase (SCD) Inhibitor MK8245 MK 8245 inhibit inhibitor

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