| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Ro 41-1049 targets monoamine oxidase A (MAO-A), an enzyme responsible for the metabolism of several key neurotransmitters, including serotonin, norepinephrine, and dopamine. By inhibiting MAO-A, Ro 41-1049 increases the availability of these neurotransmitters, playing a crucial role in regulating mood, emotional responses, and cognitive functions. It is a reversible and selective inhibitor.
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| ln Vitro |
In vitro, Ro 41-1049 is a selective and reversible inhibitor of MAO-A. Its Kd values are 16.5 and 64.4 nM, respectively. It is a mechanism-based reversible MAO-A inhibitor with a defined ~35 min adduct half-life. Its activity is confirmed in enzyme assays using recombinant MAO-A and MAO-B.
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| ln Vivo |
In vivo, Ro 41-1049 is a reversible, selective MAO-A inhibitor. By inhibiting MAO-A, it effectively increases the availability of serotonin, norepinephrine, and dopamine in the central nervous system and peripheral tissues. Its effects on mood, emotional responses, and cognitive functions are studied.
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| Enzyme Assay |
Cell-free assays for Ro 41-1049 are MAO-A and MAO-B inhibition assays using purified enzymes. The enzyme is incubated with a substrate (e.g., kynuramine) and varying concentrations of Ro 41-1049, and the rate of substrate oxidation is measured spectrophotometrically. The IC50 or Ki for inhibition of MAO-A and MAO-B is determined.
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| Cell Assay |
Cellular assays for Ro 41-1049 are performed using cell lines expressing MAO-A or MAO-B. Cells are treated with varying concentrations of Ro 41-1049, and MAO activity is measured by assessing the metabolism of a fluorescent or radiolabeled substrate. The compound's selectivity for MAO-A is confirmed.
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| Animal Protocol |
In vivo animal experiments for Ro 41-1049 are conducted in animal models of depression and anxiety. Animals are administered Ro 41-1049 orally or intraperitoneally, and behavioral tests such as the forced swim test or elevated plus maze are performed. Neurotransmitter levels in the brain are measured.
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| ADME/Pharmacokinetics |
Ro 41-1049 has a molecular weight of 265.31 g/mol and a molecular formula of C12H12FN3OS. It is a solid powder. It is soluble in DMSO and should be stored under recommended conditions. Its chemical name is N-(2-Aminoethyl)-5-(3-fluorophenyl)thiazole-4-carboxamide.
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| Toxicity/Toxicokinetics |
The toxicological profile of Ro 41-1049 has not been extensively characterized. As a MAO-A inhibitor, it may cause side effects including headache, dizziness, and gastrointestinal disturbances. It may interact with other medications, particularly serotonergic agents. No significant toxicity has been reported.
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| References |
Culver KE, Szechtman H, Levant B. Altered dopamine D2-like receptor binding in rats with behavioral sensitization to quinpirole: effects of pre-treatment with Ro 41-1049. Eur J Pharmacol. 2008 Sep 11;592(1-3):67-72. doi: 10.1016/j.ejphar.2008.06.101. PubMed PMID: 18644362; PubMed Central PMCID: PMC2577911.
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| Additional Infomation |
Ro 41-1049 is a reversible, selective MAO-A inhibitor. It is also known as Ro-41-1049. It is a mechanism-based reversible MAO-A inhibitor with a defined ~35 min adduct half-life. It is a research compound for studying the role of MAO-A in neurotransmitter metabolism and related disorders.
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| Molecular Formula |
C12H12FN3OS
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|---|---|
| Molecular Weight |
265.31
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| Exact Mass |
301.045
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| CAS # |
127500-84-9
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| Related CAS # |
127500-84-9;
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| PubChem CID |
5086
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.312g/cm3
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| Boiling Point |
493.5ºC at 760 mmHg
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| Flash Point |
252.3ºC
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| Vapour Pressure |
7E-10mmHg at 25°C
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| Index of Refraction |
1.599
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| LogP |
3.53
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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 |
4
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| Heavy Atom Count |
18
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| Complexity |
293
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=CC(C2=C(N=CS2)C(NCCN)=O)=C1
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| InChi Key |
SCKBPXUWGMKLDM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12FN3OS/c13-9-3-1-2-8(6-9)11-10(16-7-18-11)12(17)15-5-4-14/h1-3,6-7H,4-5,14H2,(H,15,17)
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| Chemical Name |
N-(2-Aminoethyl)-5-(3-fluorophenyl)-4-thiazolecarboxamide
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| Synonyms |
Ro 41-1049 Ro-41-1049 Ro 411049.
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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) |
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
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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 | 3.7692 mL | 18.8459 mL | 37.6918 mL | |
| 5 mM | 0.7538 mL | 3.7692 mL | 7.5384 mL | |
| 10 mM | 0.3769 mL | 1.8846 mL | 3.7692 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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