| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Lazabemide (also known as Ro 19-6327; proposed trade names Pakio, Tempium) is novel, potent, selective, reversible monoamine oxidase B (MAO-B) inhibitor with IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively. Lazabemide was under development as an antiparkinsonian agent but was never marketed.
| ln Vitro |
Both radiolabeled inhibitors have high affinity for their respective enzymes and are selective ligands based on their in vitro binding characteristics. In rat cerebral cortex, 3H-Ro 19-6327 had KD and Bmax values of 18.4 nM and 3.45 pmol/mg protein, respectively [1]. Lazabemide's IC50 values are as follows: 86 μM for NA uptake, 123 μM for 5HT uptake, and >500 μM for DA uptake, respectively[1]. Human MAO-B and MAO-A are inhibited by lazabemide (5 μM) with IC50 values of 6.9 nM and >10 nM, respectively. It inhibits rat MAO-B and MAO-A in enzymatic experiments with IC50 values of 37 nM and >10 μM, respectively [2]. In terms of their capacity to trigger the release of endogenous monoamines from synaptosomes, lazabemide and L-deprenyl are not the same. Thus, compared to L-deprenyl, lazabemide (500 μM) caused a greater release of 5 HT, but it was less successful in releasing DA. On the other hand, lazabemide is essentially inert upon 5-HT and DA release [2]. In renal tubular epithelial cells treated with 50 microM L-DOPA, lazabemide (250 nM) effectively suppresses DOPAC production without increasing the concentration of freshly generated DA [3].
|
|---|---|
| ln Vivo |
Lazabemide pretreatment demonstrated lower DOPAC levels compared with comparable vehicle-treated controls, and Lazabemide (3 mg/kg) inhibited ischemia-reperfusion-induced hydroxyl radical generation [4].
|
| References |
[1]. Saura J, et al. Quantitative enzyme radioautography with 3H-Ro 41-1049 and 3H-Ro 19-6327 in vitro: localization and abundance of MAO-A and MAO-B in rat CNS, peripheral organs, and human brain. J Neurosci. 1992 May;12(5):1977-99.
[2]. Bondiolotti GP, et al. In vitro effects on monoamine uptake and release by the reversible monoamine oxidase-B inhibitors lazabemide and N-(2-aminoethyl)-p-chlorobenzamide: a comparison with L-deprenyl. Biochem Pharmacol. 1995 Jun 29;50(1):97-102. [3]. Guimaraes J, et al. The activity of MAO A and B in rat renal cells and tubules. Life Sci. 1998;62(8):727-37. [4]. Suzuki T, et al. MAO inhibitors, clorgyline and lazabemide, prevent hydroxyl radical generation caused by brain ischemia/reperfusion in mice. Pharmacology. 1995 Jun;50(6):357-62. |
| Molecular Formula |
C8H10N3OCL
|
|---|---|
| Molecular Weight |
199.6375
|
| CAS # |
103878-84-8
|
| Related CAS # |
Lazabemide hydrochloride;103878-83-7
|
| SMILES |
ClC1=CC=C(C(NCCN)=O)N=C1
|
| Synonyms |
Ro 19-6327; Ro-19-6327; Ro 19 6327
|
| 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) |
DMSO : ~5 mg/mL (~25.05 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (2.50 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 5.0 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: ≥ 0.5 mg/mL (2.50 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 5.0 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. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (2.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0090 mL | 25.0451 mL | 50.0902 mL | |
| 5 mM | 1.0018 mL | 5.0090 mL | 10.0180 mL | |
| 10 mM | 0.5009 mL | 2.5045 mL | 5.0090 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA