Lazabemide HCl (Ro 19-6327 HCl) is a selective and reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM), but has low activity against MAO-A (IC50>100 μM). Lazabemide at high concentrations has the effect of inhibiting monoamine uptake. The IC50s for inhibiting the uptake of norepinephrine, serotonin and dopamine are 86 μM, 123 μM and >500 μM respectively. Lazabemide may be used in research into Parkinson's and AD/Alzheimer's diseases.

Physicochemical Properties

Molecular Formula	C8H11CL2N3O
Molecular Weight	236.10
Exact Mass	235.028
CAS #	103878-83-7
Related CAS #	Lazabemide;103878-84-8
PubChem CID	163727
Appearance	Typically exists as solid at room temperature
Boiling Point	397.4ºC at 760mmHg
Flash Point	194.2ºC
Vapour Pressure	1.59E-06mmHg at 25°C
LogP	2.316
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	14
Complexity	177
Defined Atom Stereocenter Count	0
SMILES	C1=CC(=NC=C1Cl)C(=O)NCCN.Cl
InChi Key	JMFKTFLARGGXCC-UHFFFAOYSA-N
InChi Code	InChI=1S/C8H10ClN3O.ClH/c9-6-1-2-7(12-5-6)8(13)11-4-3-10;/h1-2,5H,3-4,10H2,(H,11,13);1H
Chemical Name	N-(2-aminoethyl)-5-chloropyridine-2-carboxamide;hydrochloride
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	MAO-B 0.4 nM (IC50)
ln Vitro	Both radiolabeled inhibitors were found to be selective, high-affinity ligands for their respective enzymes based on their in vitro binding properties. In the rat cerebral cortex, the KD and Bmax values for 3H-Ro 19-6327 are 18.4 nM and 3.45 pmol/mg protein, respectively [1]. Lazabemide's IC50 values are as follows: > 500 μM for DA uptake, 86 μM for NA uptake, and 123 μM for 5HT uptake[1]. ..Human MAO-B and MAO-A are inhibited by lazabemide (5 μM) with IC50 values of 6.9 nM and >10 nM, respectively. Additionally, in an enzymatic assay, it inhibits rat MAO-B and MAO-A with IC50 values of 37 nM and >10 μM, respectively[2]. cause synaptosomes to release endogenous monoamines. Therefore, compared to L-deprenyl, lazabemide (500 μM) causes a larger release of 5 HT, but it releases DA less efficiently. Conversely, on both 5 HT and DA release, lazabemide was essentially inert[2]. When tubular epithelial cells are treated with 50 microM L-DOPA, lazabemide (250 nM) clearly inhibits the production of DOPAC but does not increase the accumulation of newly-formed DA[3].
ln Vivo	Lazabemide (3 mg/kg) reduces the production of hydroxyl radicals caused by ischemia reperfusion, and pretreatment with the drug resulted in lower DOPAC levels compared to the vehicle-treated control groups[4].
References	[1]. 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]. 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]. The activity of MAO A and B in rat renal cells and tubules. Life Sci. 1998;62(8):727-37. [4]. MAO inhibitors, clorgyline and lazabemide, prevent hydroxyl radical generation caused by brain ischemia/reperfusion in mice. Pharmacology. 1995 Jun;50(6):357-62.
Additional Infomation	Lazabemide hydrochloride is a pyridinecarboxamide.

Solubility Data

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

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.2355 mL	21.1775 mL	42.3549 mL
	5 mM	0.8471 mL	4.2355 mL	8.4710 mL
	10 mM	0.4235 mL	2.1177 mL	4.2355 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.