Saclofen
CAS No. : 125464-42-8
| Size | Price | Stock |
|---|---|---|
| 5mg | $150 | In-stock |
| 10mg | $240 | In-stock |
| 25mg | $460 | In-stock |
| 50mg | $740 | In-stock |
| 100mg | $1180 | In-stock |
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| Cat. No. : | HY-100813 |
| M.Wt: | 249.72 |
| Formula: | C9H12ClNO3S |
| Purity: | >98 % |
| Solubility: | H2O : 10 mg/mL (ultrasonic) |
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[1][2][3][4][5].
In Vitro: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].
In Vivo:Saclofen (50 μg/10 μL/rat, i.c.) 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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