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MedKoo Cat#: 525429 | Name: Lazabemide free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lazabemide is a reversible and selective inhibitor of monoamine oxidase B (MAO-B). Lazabemide is potentially an antiparkinsonian agent.

Chemical Structure

Lazabemide free base
Lazabemide free base
CAS#103878-84-8 (free base)

Theoretical Analysis

MedKoo Cat#: 525429

Name: Lazabemide free base

CAS#: 103878-84-8 (free base)

Chemical Formula: C8H10ClN3O

Exact Mass: 199.0512

Molecular Weight: 199.64

Elemental Analysis: C, 48.13; H, 5.05; Cl, 17.76; N, 21.05; O, 8.01

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
50mg USD 650.00 2 Weeks
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Related CAS #
103878-83-7 (HCl) 103878-84-8 (free base)
Synonym
Lazabemide; Ro 19-6327/000; Ro19-6327/000; Ro-19-6327/000;
IUPAC/Chemical Name
6-Chloropyridine-N-(3-hydroxypropyl)-2-carbonylamide
InChi Key
JZXRLKWWVNUZRB-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H10ClN3O/c9-6-1-2-7(12-5-6)8(13)11-4-3-10/h1-2,5H,3-4,10H2,(H,11,13)
SMILES Code
O=C(C1=NC=C(Cl)C=C1)NCCN
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 103878-83-7 (Lazabemide hydrochloride) 103878-84-8 (Lazabemide)
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM).
In vitro activity:
Under physiologic-like conditions, lazabemide inhibited lipid peroxidation in a highly concentration-dependent manner. At low, pharmacologic levels of lazabemide (100.0 nM), there was a significant (P < 0.001) and catalytic reduction in lipid peroxide formation, as compared with control samples. The antioxidant activity of lazabemide was significantly more effective than that of either vitamin E or the MAO-B inhibitor, selegiline. Reference: Biochem Pharmacol. 2000 Sep 1;60(5):709-16. https://pubmed.ncbi.nlm.nih.gov/10927030/
In vivo activity:
The ischemia reperfusion-induced hydroxyl radical generation was attenuated by 3 mg/kg of clorgyline and lazabemide. Furthermore, mice pretreated with these MAO inhibitors showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups; recovery of the reduced DOPAC level was also delayed. Reference: Pharmacology. 1995 Jun;50(6):357-62. https://pubmed.ncbi.nlm.nih.gov/7568334/
Solvent mg/mL mM
Solubility
DMSO 5.0 25.05
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 199.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Mason RP, Olmstead EG, Jacob RF. Antioxidant activity of the monoamine oxidase B inhibitor lazabemide. Biochem Pharmacol. 2000 Sep 1;60(5):709-16. doi: 10.1016/s0006-2952(00)00374-9. PMID: 10927030. 2. Guimarães JT, Soares-da-Silva P. The activity of MAO A and B in rat renal cells and tubules. Life Sci. 1998;62(8):727-37. doi: 10.1016/s0024-3205(97)01171-5. PMID: 9489509.
In vitro protocol:
1. Mason RP, Olmstead EG, Jacob RF. Antioxidant activity of the monoamine oxidase B inhibitor lazabemide. Biochem Pharmacol. 2000 Sep 1;60(5):709-16. doi: 10.1016/s0006-2952(00)00374-9. PMID: 10927030. 2. Guimarães JT, Soares-da-Silva P. The activity of MAO A and B in rat renal cells and tubules. Life Sci. 1998;62(8):727-37. doi: 10.1016/s0024-3205(97)01171-5. PMID: 9489509.
In vivo protocol:
1. Suzuki T, Akaike N, Ueno K, Tanaka Y, Himori N. MAO inhibitors, clorgyline and lazabemide, prevent hydroxyl radical generation caused by brain ischemia/reperfusion in mice. Pharmacology. 1995 Jun;50(6):357-62. doi: 10.1159/000139304. PMID: 7568334. 2. Saura J, Kettler R, Da Prada M, Richards JG. 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. doi: 10.1523/JNEUROSCI.12-05-01977.1992. PMID: 1578281; PMCID: PMC6575899.
1: Ballesteros J, Maeztu AI, Callado LF, Meana JJ, Gutiérrez M. Specific binding of [3H]Ro 19-6327 (lazabemide) to monoamine oxidase B is increased in frontal cortex of suicide victims after controlling for age at death. Eur Neuropsychopharmacol. 2008 Jan;18(1):55-61. Epub 2007 Jun 13. PubMed PMID: 17570647. 2: Berlin I, Aubin HJ, Pedarriosse AM, Rames A, Lancrenon S, Lagrue G; Lazabemide in Smoking Cessation Study Investigators. Lazabemide, a selective, reversible monoamine oxidase B inhibitor, as an aid to smoking cessation. Addiction. 2002 Oct;97(10):1347-54. PubMed PMID: 12359039. 3: Jolkkonen J, Kauppinen R, Nyman L, Haapalinna A, Sivenius J. MAO-B inhibition by a single dose of l-deprenyl or lazabemide does not prevent neuronal damage following focal cerebral ischaemia in rats. Pharmacol Toxicol. 2000 Nov;87(5):242-5. PubMed PMID: 11129505. 4: Mason RP, Olmstead EG, Jacob RF. Antioxidant activity of the monoamine oxidase B inhibitor lazabemide. Biochem Pharmacol. 2000 Sep 1;60(5):709-16. PubMed PMID: 10927030. 5: Narabayashi H, Yamaguchi T, Sugi K, Mitamura H, Mizuno Y, Nakashima M. Safety study of lazabemide (Ro19-6327), a new MAO-B inhibitor, on cardiac arrhythmias and blood pressure of patients with Parkinson's disease. Clin Neuropharmacol. 1999 Nov-Dec;22(6):340-6. PubMed PMID: 10626094. 6: Cesura AM, Borroni E, Gottowik J, Kuhn C, Malherbe P, Martin J, Richards JG. Lazabemide for the treatment of Alzheimer's disease: rationale and therapeutic perspectives. Adv Neurol. 1999;80:521-8. Review. PubMed PMID: 10410766. 7: Dingemanse J, Wood N, Jorga K, Kettler R. Pharmacokinetics and pharmacodynamics of single and multiple doses of the MAO-B inhibitor lazabemide in healthy subjects. Br J Clin Pharmacol. 1997 Jan;43(1):41-7. PubMed PMID: 9056051. 8: Effect of lazabemide on the progression of disability in early Parkinson's disease. The Parkinson Study Group. Ann Neurol. 1996 Jul;40(1):99-107. PubMed PMID: 8687199. 9: Dingemanse J, Hussain Y, Korn A. Tyramine pharmacodynamics during combined administration of lazabemide and moclobemide. Int J Clin Pharmacol Ther. 1996 Apr;34(4):172-7. PubMed PMID: 8861736. 10: Cesura AM, Gottowik J, Lahm HW, Lang G, Imhof R, Malherbe P, Röthlisberger U, Da Prada M. Investigation on the structure of the active site of monoamine oxidase-B by affinity labeling with the selective inhibitor lazabemide and by site-directed mutagenesis. Eur J Biochem. 1996 Mar 15;236(3):996-1002. PubMed PMID: 8665924. 11: Bondiolotti GP, Galva MD, Villa F, Sciaba L, Picotti GB. 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. PubMed PMID: 7605351. 12: Suzuki T, Akaike N, Ueno K, Tanaka Y, Himori N. MAO inhibitors, clorgyline and lazabemide, prevent hydroxyl radical generation caused by brain ischemia/reperfusion in mice. Pharmacology. 1995 Jun;50(6):357-62. PubMed PMID: 7568334. 13: Davis PP, Crews T, Bradford JJ, Edom RW. Determination of Ro 19-6327 (Lazabemide) in human plasma and urine by gas chromatography-negative chemical ionization mass spectrometry. J Chromatogr B Biomed Appl. 1995 Mar 24;665(2):327-35. PubMed PMID: 7795812. 14: Galva MD, Bondiolotti GP, Olasmaa M, Picotti GB. Effect of aging on lazabemide binding, monoamine oxidase activity and monoamine metabolites in human frontal cortex. J Neural Transm Gen Sect. 1995;101(1-3):83-94. PubMed PMID: 8695059. 15: Holford NH, Guentert TW, Dingemanse J, Kettler R. Pharmacodynamics of lazabemide, a reversible and selective inhibitor of monoamine oxidase B. Br J Clin Pharmacol. 1994 Jun;37(6):553-7. PubMed PMID: 7917773; PubMed Central PMCID: PMC1364814. 16: Guentert TW, Holford NH, Pfefen JP, Dingemanse J. Mixed linear and non-linear disposition of lazabemide, a reversible and selective inhibitor of monoamine oxidase B. Br J Clin Pharmacol. 1994 Jun;37(6):545-51. PubMed PMID: 7917772; PubMed Central PMCID: PMC1364813. 17: A controlled trial of lazabemide (Ro 19-6327) in levodopa-treated Parkinson's disease. Parkinson Study Group. Arch Neurol. 1994 Apr;51(4):342-7. PubMed PMID: 8155011. 18: Henriot S, Kuhn C, Kettler R, Da Prada M. Lazabemide (Ro 19-6327), a reversible and highly sensitive MAO-B inhibitor: preclinical and clinical findings. J Neural Transm Suppl. 1994;41:321-5. PubMed PMID: 7931245. 19: LeWitt PA, Segel SA, Mistura KL, Schork MA. Symptomatic anti-parkinsonian effects of monoamine oxidase-B inhibition: comparison of selegiline and lazabemide. Clin Neuropharmacol. 1993 Aug;16(4):332-7. PubMed PMID: 8374913. 20: A controlled trial of lazabemide (RO19-6327) in untreated Parkinson's disease. Parkinson Study Group. Ann Neurol. 1993 Apr;33(4):350-6. PubMed PMID: 8489205.