[CAS NO. 127917-66-2] Ro 41-1049 hydrochloride
PRODUCTS SPECIFICATIONS [127917-66-2]
DESCRIPTION [127917-66-2]
Overview
| MDL | MFCD00900596 |
|---|---|
| Molecular Weight | 301.77 |
| Molecular Formula | C12H13ClFN3OS |
| SMILES | O=C(C1=C(C2=CC=CC(F)=C2)SC=N1)NCCN.[H]Cl |
Summary
Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A) . An homogeneous population of high affinity binding sites for [ 3 H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta ( K d values of 16.5 and 64.4 nM, respectively) [1] .
IC50 & Target
MAO-A [1]
In Vivo
Ro 41-1049 (1-50 mg/kg; intraperitoneal injection; for 3 hours; Sprague-Dawley rats) treatment inhibits dopamine metabolite formation and increases dopamine levels in a dose-dependent fashion. Pretreatment with Ro 41-1049 (20 mg/kg) significantly increases dopamine formation following L-dopa administration (100 mg/kg IP) while decreasing formation of 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Sprague-Dawley rats (200-240 g) [2] |
| Dosage: | 1 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, or 50 mg/kg |
| Administration: | Intraperitoneal injection; for 3 hours |
| Result: | Inhibited dopamine metabolite formation and increased dopamine levels in a dose-dependent fashion. Pretreatment with the concentration of 20 mg/kg significantly increased dopamine formation following L-dopa administration while decreasing formation of DOPAC and HVA. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 32 mg/mL ( 106.04 mM )
H 2 O : 25 mg/mL ( 82.84 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
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1.
Add each solvent one by one: PBS
Solubility: 20 mg/mL (66.28 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.28 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.28 mM); Clear solution
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.
