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MRK-016

Name: MRK-016
Brand: TargetMol
SKU: T12105
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12105Cas No. 342652-67-9

Alias MRK016

MRK-016 is a selective GABAA α5 receptor inverse agonist/ negative allosteric modulator, (IC50=3 nM) with the advantages of being orally available and penetrating the blood-brain barrier.MRK-016 increases long time period potentiation (LTP) in mouse hippocampal slices, with memory-improvement, antidepressant, and pain-treating effects.

MRK-016

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Purity: 99.76%

Catalog No. T12105Alias MRK016Cas No. 342652-67-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$42	-	In Stock
5 mg	$98	-	In Stock
10 mg	$156	-	In Stock
25 mg	$263	-	In Stock
50 mg	$347	-	In Stock
1 mL x 10 mM (in DMSO)	$108	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.76%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	MRK-016 is a selective GABAA α5 receptor inverse agonist/ negative allosteric modulator, (IC50=3 nM) with the advantages of being orally available and penetrating the blood-brain barrier.MRK-016 increases long time period potentiation (LTP) in mouse hippocampal slices, with memory-improvement, antidepressant, and pain-treating effects.
Targets&IC50	GABAA α5:3 nM (EC50), GABAA α3β3γ2 (human):0.77 nM (Ki), GABAA α2β3γ2 (human):0.85 nM (Ki), GABAA α5β3γ2 (human):1.4 nM (Ki), GABAA α1β3γ2 (human):0.83 nM (Ki)
In vitro	MRK-016 is a selective, orally bioavailable inverse MARKET α5 receptor agonist.[1]
In vivo	MRK-016 (0.3, 1 or 3 mg/kg, oral) exhibits cognitive enhancement activity in the delayed matching place version of the Morris water maze. [2] MRK-016 (3 mg/kg, intraperitoneal) prevents LPS-induced learning/memory impairment in mice. [3]
Synonyms	MRK016

Chemical Properties

Molecular Weight	368.39
Formula	C₁₇H₂₀N₈O₂
Cas No.	342652-67-9
Smiles	N=1N=C(C2=NOC(=C2)C)N3N=C(OCC4=NC=NN4C)C(=C3C1)C(C)(C)C
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (108.58 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.43 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7145 mL	13.5726 mL	27.1451 mL	135.7257 mL
5 mM	0.5429 mL	2.7145 mL	5.4290 mL	27.1451 mL
10 mM	0.2715 mL	1.3573 mL	2.7145 mL	13.5726 mL
20 mM	0.1357 mL	0.6786 mL	1.3573 mL	6.7863 mL
50 mM	0.0543 mL	0.2715 mL	0.5429 mL	2.7145 mL
100 mM	0.0271 mL	0.1357 mL	0.2715 mL	1.3573 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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