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Saclofen

CAT: 0804-HY-100813-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-100813-01Size:5 mg
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Description
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 to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats[1][2][3][4][5].
CAS Number
125464-42-8
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
GABA Receptor
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Inflammation/Immunology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/saclofen.html
Purity
99.70
Solubility
H2O : 10 mg/mL (ultrasonic)
Smiles
O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
Molecular Formula
C9H12ClNO3S
Molecular Weight
249.72
Precautions
H302, H315, H319, H335
References & Citations
[1]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. |[2]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.|[3]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.|[4]Seyyed Hamid Bathaei, et al. The Effect of Flavonoids Catechin, Baclofen and Saclofen on Acetic Acid - Induced Visceral Pain by in Rat. International Journal of Pharmaceutical Research & Allied Sciences. 2016, 5 (1) :81-85|[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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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