| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
RS-8359 targets monoamine oxidase A (MAO-A), a mitochondrial enzyme responsible for the degradation of monoamine neurotransmitters such as serotonin, norepinephrine, and dopamine. It is a selective and reversible MAO-A inhibitor with a selectivity ratio of about 2200 for the A:B enzyme types. By inhibiting MAO-A, RS-8359 enhances neurotransmission by preventing the degradation of monoamine neurotransmitters. This mechanism is responsible for its antidepressant activity. The compound shows relatively little effect on blood pressure when administered with tyramine, indicating a reduced risk of hypertensive crisis.
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| ln Vitro |
In vitro, RS-8359 is a selective and reversible inhibitor of MAO-A with a selectivity ratio of about 2200 for the A:B enzyme types. It has low affinity for common central nervous system receptors and minimal anticholinergic effects. The compound's ability to inhibit MAO-A-mediated degradation of monoamine neurotransmitters has been confirmed in enzyme assays. Its selectivity for MAO-A over MAO-B makes it a valuable tool for studying the specific role of MAO-A in neurological and psychiatric disorders.
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| ln Vivo |
The blood pressure response to RS 8359 in combination with tyramine is comparatively mild. According to a study, RS-8359 exhibits low anticholinergic effects and low affinity for common central nervous system [1].
In vivo, RS-8359 has demonstrated antidepressant activity in animal models. It shows relatively little effect on blood pressure when administered together with tyramine, effectively eliminating the "cheese effect" that limits the clinical use of classical MAO inhibitors. The compound's low affinity for common CNS receptors and minimal anticholinergic effects suggest a favorable side-effect profile. RS-8359 has been developed for mood and anxiety disorders. |
| Enzyme Assay |
In vitro enzyme assays for RS-8359 measure its inhibition of MAO-A and MAO-B activity. MAO enzymes are incubated with a substrate (e.g., serotonin or benzylamine) in the presence of varying concentrations of RS-8359. The production of the oxidative deamination product is measured spectrophotometrically or by HPLC. The IC50 for MAO-A inhibition is determined, and the selectivity ratio for MAO-A over MAO-B is calculated (approximately 2200). These assays confirm the compound's potent and selective MAO-A inhibitory activity.
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| Cell Assay |
In vitro cell-based assays for RS-8359 are used to study its effects on neurotransmitter metabolism in neuronal cells. Neuronal cell lines or primary neuronal cultures are treated with RS-8359, and the levels of monoamine neurotransmitters (serotonin, norepinephrine, dopamine) and their metabolites are measured by HPLC or LC-MS/MS. The compound's ability to increase neurotransmitter levels by inhibiting MAO-A-mediated degradation is assessed. Cytotoxicity is evaluated using standard viability assays to ensure that the observed effects are not due to cell death.
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| Animal Protocol |
In vivo animal experiments for RS-8359 are conducted in animal models of depression, such as the forced swim test or tail suspension test in rodents. RS-8359 is administered orally or intraperitoneally, and the reduction in immobility time is measured as an indicator of antidepressant activity. The compound's effects on blood pressure when co-administered with tyramine are also assessed to evaluate the risk of the "cheese effect". These studies confirm the antidepressant activity and favorable safety profile of RS-8359.
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| ADME/Pharmacokinetics |
RS-8359 has a molecular weight of 252.27 g/mol and a molecular formula of C14H12N4O. It has a predicted density of 1.39 g/cm3. The compound is a white solid with a purity of 99.3%. It is soluble in DMSO at 48 mg/mL (190.27 mM) with sonication and heating to 80°C recommended. For storage, it is recommended to keep the powder at -20°C for up to 3 years. In solvent, it can be stored at -80°C for 1 year. The compound is shipped with blue ice or at ambient temperature. Detailed pharmacokinetic properties such as half-life and bioavailability have been characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for RS-8359 is not extensively detailed in standard product descriptions. The compound shows relatively little effect on blood pressure when administered with tyramine, effectively eliminating the "cheese effect" that limits the clinical use of classical MAO inhibitors. It has low affinity for common central nervous system receptors and minimal anticholinergic effects, suggesting a favorable safety profile. However, as with all MAO inhibitors, caution should be exercised regarding potential drug interactions and dietary restrictions. As with all research chemicals, standard laboratory safety precautions should be followed when handling RS-8359.
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| References | |
| Additional Infomation |
RS-8359 is a research compound and is not approved for any clinical or therapeutic use. It is a selective and reversible inhibitor of monoamine oxidase A (MAO-A) with a selectivity ratio of about 2200 for the A:B enzyme types. RS-8359 has antidepressant activity and shows relatively little effect on blood pressure when administered together with tyramine, effectively eliminating the "cheese effect". It has low affinity for common CNS receptors and minimal anticholinergic effects. The compound has been developed for mood and anxiety disorders. Its mechanism of action involves inhibiting MAO-A-mediated degradation of monoamine neurotransmitters.
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| Molecular Formula |
C14H12N4O
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| Molecular Weight |
252.277
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| Exact Mass |
252.101
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| CAS # |
105365-76-2
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| PubChem CID |
164116
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
483.6±45.0 °C at 760 mmHg
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| Flash Point |
246.3±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.682
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| LogP |
1.12
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
358
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YKTSVZRWKHWINV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12N4O/c15-7-9-1-3-10(4-2-9)18-14-11-5-6-12(19)13(11)16-8-17-14/h1-4,8,12,19H,5-6H2,(H,16,17,18)
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| Chemical Name |
4-[(7-hydroxy-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino]benzonitrile
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| Synonyms |
RS-8359 RS8359 RS 8359
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~198.20 mM)
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| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9638 mL | 19.8192 mL | 39.6385 mL | |
| 5 mM | 0.7928 mL | 3.9638 mL | 7.9277 mL | |
| 10 mM | 0.3964 mL | 1.9819 mL | 3.9638 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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