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A7201412

Rasagiline , 97% , 136236-51-6

CAS NO.:136236-51-6

Empirical Formula: C12H13N

Molecular Weight: 171.24

MDL number: MFCD00866571

Pack Size Price Stock Quantity
100mg RMB159.20 In Stock
250MG RMB287.20 In Stock
1G RMB799.20 In Stock
5g RMB2959.20 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 148 °C
Boiling point: 305.5±30.0 °C(Predicted)
Density  1.05±0.1 g/cm3(Predicted)
storage temp.  under inert gas (nitrogen or Argon) at 2–8 °C
solubility  Dichloromethane
form  Solid
pka 6.95±0.20(Predicted)
color  Off-White to Light Beige to Orange
Stability: Light Sensitive
InChI InChI=1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1
InChIKey RUOKEQAAGRXIBM-GFCCVEGCSA-N
SMILES [C@H]1(NCC#C)C2=C(C=CC=C2)CC1

Description and Uses

Rasagiline is a second-generation, irreversible monoamine oxidase type B (MAO-B) inhibitor that has been launched for the treatment of Parkinson’s disease (PD). Unlike its predecessor selegiline, it is not metabolized to amphetamine derivatives and is, therefore, devoid of the sympathomimetic activity responsible for adverse side effects. Rasagiline is, however, similar to selegiline in the retention of the propargylamine moiety; this essential pharmacophore binds covalently to selectively form an irreversible bond with the flavin adenine dinucleotide portion of the MAO-B enzyme. As an adjunct therapy, rasagiline treats the fluctuations in motor symptoms. The R-enantiomer exhibits 4-times the potency of the S-enantiomer, so the synthetic method begins with the optical resolution of racemic N-benzyl-1-aminoindan using (R,R)-tartaric acid as the resolving agent. Once isolated, the enantiomerically-enriched salt is submitted to hydrogenolysis to afford 1(R)- aminoindane that is subsequently propargylated to provide rasagiline. It is formulated as its mesylate salt, and the recommended dosage of rasagiline is 1 mg/day, with or without levodopa. Entacapone, a catecholamine- O-methyltransferase inhibitor known as an effective add-on therapy for motor fluctuations, was used as a comparator. Rasagiline reduced the time spent in the “off” state while increasing the “on” time.

5HT4 receptor agonist, peristaltic stimulant. Rasagiline, is a selective and irreversible propargylamine inhibitor of monoamine oxidase which has been used to increase the availability of dopamine at striatal receptors as a method to treat Parkinson’s disease.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
HS Code  2921490090
Hazardous Substances Data 136236-51-6(Hazardous Substances Data)

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