(R)-Baclofen

Arbaclofen, also known as (R)-Baclofen, D-Baclofen and STX209, is a selective GABA-B agonist and is hypothesized to modulate the balance of excitatory to inhibitory neurotransmission, and has shown preliminary evidence of benefit in fragile X syndrome. STX209 may be a potentially effective therapy to treat the core symptoms of FXS. Autism spectrum disorder (ASD) is a behaviorally defined disorder which has increased in prevalence over the last two decades.

Product information

CAS Number: 69308-37-8

Molecular Weight: 213.66

Formula: C10H12ClNO2

Synonym:

STX 209

STX-209

STX209

Chemical Name: (3R)-4-amino-3-(4-chlorophenyl)butanoic acid

Smiles: NC[C@H](CC(O)=O)C1C=CC(Cl)=CC=1

InChiKey: KPYSYYIEGFHWSV-QMMMGPOBSA-N

InChi: InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)/t8-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 5 mg/mL (23.40 mM; Need ultrasonic) DMSO : 1 mg/mL (4.68 mM; ultrasonic and warming and heat to 80°C)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

(R)-Baclofen (STX209) suppresses audiogenic seizures in the Fmr1-knockout mouse on the seizure-resistant C57BL/6 background with an effective dose of 1 mg/kg . Acute intraperitoneal administration of (R)-Baclofen (STX209) significantly reduces the percent of mice displaying seizures (seizure incidence), with a minimum effective dose (MED) of 1.5 mg/kg.

References:

1. Falch E, Hedegaard A, Nielsen L et al. Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations. J Neurochem. 1986 Sep;47(3):898-903.
2. Henderson C, et al. Reversal of disease-related pathologies in the fragile X mouse model by selective activation of GABAB receptors with arbaclofen. Sci Transl Med. 2012 Sep 19;4(152):152ra128.
3. Hong YG, Henry JL. Effects of phaclofen and the enantiomers of baclofen on cardiovascular responses to intrathecal administration of L- and D-baclofen in the rat. Eur J Pharmacol. 1991 Apr 24;196(3):267-75.

Products are for research use only. Not for human use.