Shopping Cart
- Remove All
Your shopping cart is currently empty
MRK-016
🥰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
Catalog No. T12105Alias MRK016Cas No. 342652-67-9
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.
Product information is being updated, if you want to purchase, please click the bulk custom button.
Bulk & Custom
Questions
View MoreInhibitors Related to "MRK-016"
p-Hydroxybenzaldehyde
p-Oxybenzaldehyde, 4-hydroxybenzaldehyde, 4-Formylphenol
T2S1814123-08-0
1. p-Hydroxybenzaldehyde (p-Oxybenzaldehyde) shows an inhibitory effect on the GABA transaminase to contribute to an antiepileptic and anticonvulsive activity, and its inhibitory activity was higher than that of valproic acid, a known anticonvulsant.
- $47
Size
QTY
Riluzole
RP-54274, PK 26124
T03491744-22-5
Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
- $45
Size
QTY
Methionine
MRX-1024, D-Methionine
T19418L348-67-4
Methionine (D-Methionine) (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
- $50
Size
QTY
DL-Menthol
Hexahydrothymol, (±)-Menthol
T297989-78-1
DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.
- $42
Size
QTY
Valproic Acid
Cited
VPA, Sodium valproate, Depakine, 2-Propylvaleric Acid, 2-Propylpentanoic Acid
T706499-66-1
Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.
- $50
Size
QTY
CitedHalothane
Narcotane, Anestan
T0954151-67-7
Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.
- $45
Size
QTY
(-)-α-Pinene
(1S)-(-)-Alpha-Pinene
TN12027785-26-4
(-)-α-Pinene ((1S)-(-)-Alpha-Pinene) enhances the quantity of NREMS without affecting the intensity of NREMS by prolonging GABAergic synaptic transmission, acting as a partial modulator of GABAA-BZD receptors and directly binding to the BZD binding site of GABAA receptor.
- $30
Size
QTY
Nikethamide
N,N-Diethylnicotinamide, Corvotone, Corvin, Anacardone
T004859-26-7
Nikethamide is a stimulant which mainly influences the respiratory cycle. Widely known by its former sales name of Coramine, it was used in the mid-twentieth century as a medical countermeasure against tranquilizer overtreatments, before the advent of end
- $40
Size
QTY
Urethane Cited
Ethylurethane, Ethyl carbamate, Carbamic acid ethyl ester
T005151-79-6
Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.
- $29
Size
QTY
CitedPenicillin G sodium salt
Penicillin G Sodium, Benzylpenicillin sodium salt, Benzylpenicillin Sodium
T095869-57-8
Penicillin G sodium(Benzylpenicillin sodium) salt is a penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.
- $47
Size
QTY
Chlorothymol
NSC-406261, NSC406261, NSC 406261, AI3-00120, AI300120, AI3 00120, 4-Chloro-2-isopropyl-5-methylphenol
T2024289-68-9
Chlorothymol (AI3-00120) is a disinfectant used in oral.
- $40
Size
QTY
Valproic acid sodium salt Cited
Sodium Valproate
T16021069-66-5
Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.
- $42
Size
QTY
CitedSelect Batch
Contact us for more batch information
Resource Download
Product Introduction
Bioactivity
Chemical Properties
| 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 α1β3γ2 (human):0.83 nM (Ki), GABAA α3β3γ2 (human):0.77 nM (Ki), GABAA α2β3γ2 (human):0.85 nM (Ki), GABAA α5β3γ2 (human):1.4 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] |
| Alias | MRK016 |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (108.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
Calculator
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 . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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
Preview
Related Tags: buy MRK-016 | purchase MRK-016 | MRK-016 cost | order MRK-016 | MRK-016 chemical structure | MRK-016 in vivo | MRK-016 in vitro | MRK-016 formula | MRK-016 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2025 TargetMol Chemicals Inc. All Rights Reserved.