Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

MK-8245 [1030612-90-8]

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Katalog-Nummer HY-13070-5mg

Size : 5mg

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Telefonnummer : +1 850 650 7790

Marke : MedChemExpress

Contact local distributor :

Telefonnummer : +1 850 650 7790

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

MK-8245 Chemische Struktur

CAS. Nr. : 1030612-90-8

This product is a controlled substance and not for sale in your territory.

Based on 3 publication(s) in Google Scholar

Other Forms of MK-8245:

MK-8245 Trifluoroacetate In-stock

Beschreibung

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Klinische Studie

Molekulargewicht

467.25

Formel

C₁₇H₁₆BrFN₆O₄

CAS. Nr.

1030612-90-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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.

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

View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner
Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 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

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.
Protocol 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

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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 (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Reinheit & Dokumentation

Purity: 99.04%

Select Batch:

Data Sheet (273 KB) SDS (536 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Complete Stock Solution Preparation Table

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

MK-8245 Related Classifications

Metabolic Enzyme/Protease
Stearoyl-CoA Desaturase (SCD)

MK-8245 [1030612-90-8]

Katalog-Nummer HY-13070-5mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Other Forms of MK-8245:

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

MK-8245 Related Classifications

Keywords:

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MK-8245 [1030612-90-8]

Katalog-Nummer HY-13070-5mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Other Forms of MK-8245:

MK-8245 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

MK-8245 Related Classifications

Keywords:

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