| Targets |
IC50: 26 μM (MAO-A), 55 μM (MAO-B)[1]
MAO-A (monoamine oxidase A) and MAO-B (monoamine oxidase B). |
|---|---|
| ln Vitro |
WAY-620147 inhibits MAO-A and MAO-B with IC50 values of 26 μM and 55 μM, respectively. This dual inhibition of both MAO isoforms makes it a useful tool for studying the combined effects of MAO-A and MAO-B inhibition on monoamine neurotransmitter metabolism.
|
| ln Vivo |
As a dual MAO-A/B inhibitor, WAY-620147 has the potential to increase the levels of multiple monoamine neurotransmitters, including serotonin, dopamine, and norepinephrine. This could have broad effects on mood, cognition, and motor function. It is used in research to explore the therapeutic potential of dual MAO inhibition.
|
| Enzyme Assay |
In vitro enzyme assays are performed to evaluate the inhibitory activity of WAY-620147 against MAO-A and MAO-B. The enzymes are incubated with substrates (e.g., serotonin for MAO-A, benzylamine for MAO-B) and varying concentrations of the compound. The inhibition of enzyme activity is measured, and IC50 values are calculated from the data.
|
| Cell Assay |
Cells expressing MAO-A or MAO-B are treated with WAY-620147 to assess its cellular effects. The compound's ability to inhibit MAO activity in intact cells is measured by monitoring the metabolism of specific monoamine substrates. Its effects on neurotransmitter levels and cellular signaling are evaluated.
|
| Animal Protocol |
In vivo studies are conducted in animal models to investigate the effects of dual MAO-A/B inhibition on behavior and physiology. WAY-620147 is typically administered via systemic routes. Its effects on depressive-like behavior, anxiety, and motor function are assessed to understand the role of MAO enzymes in these processes.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for WAY-620147. As a research compound, its ADME properties would need to be characterized to guide in vivo studies. Its ability to cross the blood-brain barrier is a key consideration for CNS activity.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available. As a dual MAO inhibitor, its toxicity profile would likely include the risk of the "cheese effect" (hypertensive crisis) due to MAO-A inhibition. Standard safety assessments would be required to evaluate its potential for other adverse effects.
|
| References |
[1]. Shi L, et al. Design of novel nicotinamides as potent and selective monoamine oxidase a inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1659-64.
|
| Additional Infomation |
WAY-620147 is a research tool for studying the combined inhibition of MAO-A and MAO-B. Its dual activity makes it useful for exploring the therapeutic potential of such inhibitors in various CNS disorders. It is not approved for clinical use and is strictly for preclinical research. It is also referred to as compound 6 in some studies.
|
| Exact Mass |
313.042
|
|---|---|
| CAS # |
515866-67-8
|
| PubChem CID |
805035
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
465.4±45.0 °C at 760 mmHg
|
| Flash Point |
235.3±28.7 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.567
|
| LogP |
0.49
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
18
|
| Complexity |
272
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
HRJAFCAVJHVTOR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H16BrN3O2/c13-11-7-10(8-14-9-11)12(17)15-1-2-16-3-5-18-6-4-16/h7-9H,1-6H2,(H,15,17)
|
| Chemical Name |
5-bromo-N-(2-morpholin-4-ylethyl)pyridine-3-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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