(R)-Baclofen
Based on 2 publication(s) in Google Scholar
(R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.50%
- CAS. Nr.: 69308-37-8
- Formel: C10H12ClNO2
- Molecular Weight:213.66
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) (R)-Baclofen
More
Biologische Aktivität
GABAB receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1 μM
Compound: (-)-baclofen
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Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
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[PMID: 23428109] |
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[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 69308-37-8
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Appearance Solid
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Molecular Weight 213.66
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Formel C10H12ClNO2
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Color White to off-white
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SMILES
ClC1=CC=C([C@](CC(O)=O)([H])CN)C=C1
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Synonyms
Arbaclofen; STX209
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Mol Med Rep
The GABAB receptor agonist STX209 reverses the autism‑like behaviour in an animal model of autism induced by prenatal exposure to valproic acid. [Abstract]2022 May;25(5):154. PMID: 35244195 -
J Neurochem
Somatostatin interneurons inhibit excitatory transmission mediated by astrocytic GABAB and presynaptic GABAB and adenosine A1 receptors in the hippocampus. [Abstract]2022 Nov;163(4):310-326. PMID: 35775994
Lösungsmittel & Löslichkeit
H2O : 5 mg/mL (23.40 mM; Need ultrasonic)
DMSO : 1 mg/mL (4.68 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 4.17 mg/mL (19.52 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Hong YG, et al. 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. [Content Brief]
[2]. Falch E, 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. [Content Brief]
[3]. Falch E, 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. [Content Brief]
[4]. Orsnes G, et al. The effect of baclofen on the transmission in spinal pathways in spastic multiple sclerosis patients. Clin Neurophysiol. 2000 Aug;111(8):1372-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.6802 mL | 23.4012 mL | 46.8025 mL | 117.0061 mL |
| H2O | 5 mM | 0.9360 mL | 4.6802 mL | 9.3605 mL | 23.4012 mL |
| 10 mM | 0.4680 mL | 2.3401 mL | 4.6802 mL | 11.7006 mL | |
| 15 mM | 0.3120 mL | 1.5601 mL | 3.1202 mL | 7.8004 mL | |
| 20 mM | 0.2340 mL | 1.1701 mL | 2.3401 mL | 5.8503 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
(R)-Baclofen Related Classifications
HY-17354 Related Classifications
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