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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameSACLOFEN
SynonymsSACLOFEN
SACLOFEN SELECTIVE GABA(B) REC
3-AMINO-2-(4-CHLOROPHENYL)-PROPANE SULFONIC ACID
3-AMino-2-(4-chlorophenyl)propane-1-sulfonic acid
(RS)-3-amino-2-(4-chlorophenyl)propylsulfonic acid

Synonyms

SACLOFEN
SACLOFEN SELECTIVE GABA(B) REC
3-AMINO-2-(4-CHLOROPHENYL)-PROPANE SULFONIC ACID
3-AMino-2-(4-chlorophenyl)propane-1-sulfonic acid
(RS)-3-amino-2-(4-chlorophenyl)propylsulfonic acid
β-(aminomethyl)-4-chlorobenzeneethanesulfonic acid
(RS)-3-AMINO-2-(4-CHLOROPHENYL)PROPYLSULFONIC ACID
BETA-(AMINOMETHYL)-4-CHLOROBENZENEETHANESULFONIC ACID
BETA-(AMINOMETHYL)-4-CHLORO-BENZENEETHANESULPHONIC ACID
CAS125464-42-8
EINECS
Chemical FormulaC9H12ClNO3S
Molecular Weight249.71
inchiInChI=1/C9H12ClNO3S/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H,12,13,14)
Package1 mg;5 mg;10 mg;25 mg
PriceEmail to quote
DescriptionsSaclofen

Saclofen

MedChemExpress (MCE)

HY-100813

125464-42-8

99.87%

Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Room temperature in continental US

Descriptions

Saclofen

Saclofen

MedChemExpress (MCE)

HY-100813

125464-42-8

99.87%

Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Room temperature in continental US
may vary elsewhere.

Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats.

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].

Saclofen (5mg/mL, i.g., single dose) improves inflammation in rats induced by lipopolysaccharides[3]. Saclofen (1mg/mL, i.p., single dose) has analgesic effects in a rat pain model induced by acetic acid[4].

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[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]

[4].

Supplier Websitehttps://www.medchemexpress.com/saclofen.html
Last Update2025-05-21 16:50:25
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