[CAS NO. 136236-51-6] Rasagiline

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PRODUCTS SPECIFICATIONS [136236-51-6]

Catalog

SLK-S5795

Brand

Selleck

CAS

136236-51-6

DESCRIPTION [136236-51-6]

Overview

MDL	MFCD00866571
Molecular Weight	171.24
Molecular Formula	C12H13N
SMILES	N(CC#C)[C@H]1C=2C(CC1)=CC=CC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Rasagiline (TVP-1012) is a novel selective and irreversible propargylamine inhibitor with in vitro IC50s of 4.43 nM and 412 nM for MAO-B and MAO-A, respectively.

Targets

MAO-B ^[1]	MAO-A ^[1]
4.43 nM	412 nM

In vitro

Rasagiline is a highly selective and potent propargylamine inhibitor of monoamine oxidase (MAO) type B. Like other similar propargylamine inhibitors, rasagiline binds covalently to the N5 nitrogen of the flavin residue of MAO, resulting in irreversible inactivation of the enzyme. Rasagiline possesses a similar degree of selectivity to selegiline for inhibition of MAO-B as compared with MAO-A, in rat hepatic and brain tissue both in vivo and in vitro. Both inhibitors will inhibit the A form of the enzyme at higher doses.

In vivo

Rasagiline is well absorbed after oral administration and readily crosses the BBB. The oral bioavailability of rasagiline is 35%, it reaches Tmax after 0.5-1 hours and its half-life is 1.5-3.5 hours. It exerts linear absorption at doses of 1-10 mg/day. Rasagiline undergoes extensive hepatic metabolism primarily by cytochrome P450 type 1A2 (CYP1A2). Plasma albumin binding is considered to be 60%-70%.

References

[1] Shimon Lecht, et al. Ther Clin Risk Manag. 2007, 3(3): 467-474.
[2] John P.M. Finberg. Rambam Maimonides Med J. 2010, 1(1): e0003.

Synonyms

1H-Inden-1-amine, 2,3-dihydro-N-2-propyn-1-yl-, (1R)-

1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (R)-

1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (1R)-

(1R)-2,3-Dihydro-N-2-propyn-1-yl-1H-inden-1-amine

Rasagiline

(R)-N-2-Propynyl-1-indanamine

(R)-(+)-Rasagiline

Azilect

R-(+)-N-Propargyl-1-aminoindan

(1R)-N-Prop-2-ynyl-2,3-dihydro-1H-inden-1-amine

(R)-N-(2-Propynyl)-2,3-dihydroinden-1-amine

(1R)-N-(Prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine

(R)-N-(Prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine