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MRK-016

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

🥰Excellent

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

🥰Excellent

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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Batch Information

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Purity:99.76%

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 α3β3γ2 (human):0.77 nM (Ki), GABAA α1β3γ2 (human):0.83 nM (Ki), GABAA α5β3γ2 (human):1.4 nM (Ki), GABAA α5:3 nM (EC50), GABAA α2β3γ2 (human):0.85 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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