RO-41-1049 hydrochloride

Alias: RO-41-1049 hydrochloride; RO 41-1049 hydrochloride; RO-41-1049 HCl.
Cat No.:V2066 Purity: ≥98%
Ro 41-1049 hydrochloride, the hydrochloride salt ofRo 41-1049, is a novel, potent, selective, reversible and orally bioavailable inhibitor of MAO-A (Monoamine oxidase).
RO-41-1049 hydrochloride Chemical Structure CAS No.: 127917-66-2
Product category: Monoamine Oxidase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of RO-41-1049 hydrochloride:

  • Ro 41-1049
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ro 41-1049 hydrochloride, the hydrochloride salt of Ro 41-1049, is a novel, potent, selective, reversible and orally bioavailable inhibitor of MAO-A (Monoamine oxidase).

Biological Activity I Assay Protocols (From Reference)
ln Vivo
Dopamine levels are dose-dependently increased and dopamine metabolite production is inhibited in Sprague-Dawley rats treated with Ro 41-1049 (1-50 mg/kg; i.p.; 3 hours). Pretreatment with Ro 41-1049 (20 mg/kg) reduced the synthesis of 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) and considerably boosted the generation of dopamine following levodopa delivery (100 mg/kg IP)[2].
Animal Protocol
Animal/Disease Models: SD (SD (Sprague-Dawley)) rat (200-240 g) [2]
Doses: 1 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg or 50 mg/kg
Route of Administration: intraperitoneal (ip) injection; 3 hour
Experimental Results: Inhibits dopamine metabolite formation and increases dopamine levels in a dose-dependent manner. Pretreatment at a concentration of 20 mg/kg Dramatically increased dopamine formation after levodopa administration while reducing DOPAC and HVA formation.
References
[1]. Cesura AM, et al. Characterization of the binding of [3H]Ro 41-1049 to the active site of human monoamine oxidase-A. Mol Pharmacol. 1990 Mar;37(3):358-66.
[2]. Brannan T, et al. Effect of a selective MAO-A inhibitor (Ro 41-1049) on striatal L-dopa and dopamine metabolism: an in vivo study. J Neural Transm Park Dis Dement Sect. 1994;8(1-2):99-105.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H13CLFN3OS
Molecular Weight
301.767523527145
CAS #
127917-66-2
Related CAS #
127500-84-9; 127917-66-2 (HCl)
SMILES
O=C(C1=C(C2=CC=CC(F)=C2)SC=N1)NCCN.[H]Cl
InChi Key
RRNSPXUFTKJIEZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H12FN3OS.ClH/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);1H
Chemical Name
4-Thiazolecarboxamide, N-(2-aminoethyl)-5-(3-fluorophenyl)-, hydrochloride (1:1)
Synonyms
RO-41-1049 hydrochloride; RO 41-1049 hydrochloride; RO-41-1049 HCl.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 32 mg/mL (~106.04 mM)
H2O : ~25 mg/mL (~82.84 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (8.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (8.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 20 mg/mL (66.28 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3138 mL 16.5689 mL 33.1378 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL
10 mM 0.3314 mL 1.6569 mL 3.3138 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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