Saclofen
Based on 5 publication(s) in Google Scholar
Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats.
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- Pureza: 99.97%
- No. CAS: 125464-42-8
- Fòrmula: C9H12ClNO3S
- Peso molecular:249.72
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Saclofen
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Actividad biológica
Saclofen (300 μM, 0-24 h) inhibits the phase changes in the circadian rhythm caused by Baclofen in brain slices of the rat suprachiasmatic nucleus (SCN) [1].
Saclofen (0.1 μM-1 mM, 10 s) suppresses the increase in CHO intracellular calcium induced by GABA at high concentrations[2].
Saclofen inhibits the binding of Baclofen to rat cerebellar membranes with an IC50 of 7.8 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Saclofen (1mg/mL, i.p., single dose) has analgesic effects in a rat pain model induced by acetic acid[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Wistar rats induced by lipopolysaccharide(LPS)[3]
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Dosage:50 μg/10 μL/rat
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Administration:i.c.
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Result:Eliminated the hypotensive effect of lipopolysaccharide (LPS), restored mean arterial pressure (MAP), and reduced the increase of TNF-α and IL-6 induced by LPS.
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Animal Model:Acetic acid -induced visceral pain by in rat[4]
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Dosage:1 mg/kg, single dose
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Administration:Intraperitoneal injection (i.p.)
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Result:Could prevent pain caused by the GABAB receptor agonist baclofen.
Chemical Information
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No. CAS 125464-42-8
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Appearance Solid
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Peso molecular 249.72
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Fòrmula C9H12ClNO3S
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Color White to off-white
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SMILES
O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 May 15;16(1):4521. PMID: 40374633 -
J Adv Res
Gut microbial GABAergic signaling improves stress-associated innate immunity to respiratory viral infection. [Abstract]2024 Jun:60:41-56. PMID: 37353002 -
Toxicol Sci
Perfluorooctanesulfonic acid (PFOS) antagonizes gamma-aminobutyric acid (GABA) receptors in larval zebrafish and mammalian models. [Abstract]2025 Jul 23:kfaf101. PMID: 40700607 -
Biochem Biophys Res Commun
2023 Nov 12:681:80-89. PMID: 37774573 -
Solvente y solubilidad
H2O : 10 mg/mL (40.04 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. K R Biggs, et al. GABAB receptor stimulation phase-shifts the mammalian circadian clock in vitro. Brain Res. 1998 Oct 5;807(1-2):250-4. [Content Brief]
[2]. M D Wood, et al. The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Br J Pharmacol. 2000 Nov;131(6):1050-4. [Content Brief]
[3]. Sallam MY, et al. Central GABAA receptors are involved in inflammatory and cardiovascular consequences of endotoxemia in conscious rats. Naunyn Schmiedebergs Arch Pharmacol. 2016 Mar;389(3):279-88. [Content Brief]
[5]. C A Drew, et al. Inhibition of baclofen binding to rat cerebellar membranes by phaclofen, saclofen, 3-aminopropylphosphonic acid and related GABAB receptor antagonists. Neurosci Lett. 1990 May 18;113(1):107-10. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.0045 mL | 20.0224 mL | 40.0449 mL | 100.1121 mL |
| 5 mM | 0.8009 mL | 4.0045 mL | 8.0090 mL | 20.0224 mL | |
| 10 mM | 0.4004 mL | 2.0022 mL | 4.0045 mL | 10.0112 mL | |
| 15 mM | 0.2670 mL | 1.3348 mL | 2.6697 mL | 6.6741 mL | |
| 20 mM | 0.2002 mL | 1.0011 mL | 2.0022 mL | 5.0056 mL | |
| 25 mM | 0.1602 mL | 0.8009 mL | 1.6018 mL | 4.0045 mL | |
| 30 mM | 0.1335 mL | 0.6674 mL | 1.3348 mL | 3.3371 mL | |
| 40 mM | 0.1001 mL | 0.5006 mL | 1.0011 mL | 2.5028 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.
Saclofen Related Classifications
HY-100813 Related Classifications
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