| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
(R)-baclofen (formerly STX-209; STX209; STX 209), a derivative of gamma-aminobutyric acid, is a selective GABAB receptor agonist that has been primarily used to treat spasticity. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing. It acts at spinal and supraspinal sites, reducing excitatory transmission. GABAB receptors are metabotropic receptors which produce slow inhibitory signals.
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| ln Vivo |
At an effective dose of 1 mg/kg, (R)-Baclofen (STX209) reduces audiogenic seizures in Fmr1-knockout mice on a seizure-resistant C57BL/6 background [5]. With a minimum effective dosage (MED) of 1.5 mg/kg, acute intraperitoneal administration of (R)-Baclofen (STX209) considerably decreased the percentage of mice having seizures (seizure incidence) [5].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Unlike baclofen, absorption of arbaclofen is not limited to the upper small intestine. Arbaclofen can also be absorbed in the lower small intestine and the colon, allowing for the development of sustained release formulations. >80% of R-baclofen is renally eliminated unchanged. Blood clearance of an IV bolus of R-baclofen in rats, monkeys, and dogs, resulted in a half life of 1.6-3.4hours, in one study. Total blood clearance was reported to be 0.51±0.13L/h/kg in rats, 0.31±0.11L/h/kg in monkeys, and 0.24±0.01L/h/kg in dogs. (2) |
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| Additional Infomation |
Arbaclofen is an organooxygen compound and an organonitrogen compound. It is functionally related to a gamma-amino acid.
Arbaclofen, or STX209, is the R-enantiomer of baclofen. It is believed to be a selective gamma-amino butyric acid type B receptor agonist, and has been investigated as a treatment for autism spectrum disorder and fragile X syndrome in randomized, double blind, placebo controlled trials. It has also been investigated as a treatment for spasticity due to multiple sclerosis and spinal cord injury. Arbaclofen was investigated as a treatment for gastroesophageal reflux disease (GERD); however, with disappointing results. Drug Indication Investigated in clinical trials as a potential treatment for spasticity in multiple sclerosis, autism spectrum disorder, and social withdrawal in fragile X syndrome. Mechanism of Action Arbaclofen, or R-baclofen, acts upstream of the mGluR5 receptor to increase inhibitory neurotransmission. It is the isomer of baclofen which harbors antispastic activity. |
| Molecular Formula |
C10H12CLNO2
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| Molecular Weight |
213.66
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| Exact Mass |
213.055
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| CAS # |
69308-37-8
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| Related CAS # |
63701-55-3
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| PubChem CID |
44602
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
364.3±32.0 °C at 760 mmHg
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| Melting Point |
171-174°C
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| Flash Point |
174.1±25.1 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
1.56
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
191
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC(=CC=C1[C@@H](CC(=O)O)CN)Cl
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| InChi Key |
KPYSYYIEGFHWSV-QMMMGPOBSA-N
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| InChi Code |
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
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| Chemical Name |
(3R)-4-amino-3-(4-chlorophenyl)butanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 4.17 mg/mL (19.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6803 mL | 23.4017 mL | 46.8033 mL | |
| 5 mM | 0.9361 mL | 4.6803 mL | 9.3607 mL | |
| 10 mM | 0.4680 mL | 2.3402 mL | 4.6803 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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