Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SX-3228 is a selective agonist of benzodiazepine1 (BZ1) receptor(IC50 of 17 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | SX-3228 is a selective agonist of benzodiazepine1 (BZ1) receptor(IC50 of 17 nM). |
Targets&IC50 | BZ1 receptor:17 nM |
In vitro | SX-3228 is a selective ligand for the BZ1 receptor. Among the BZ-receptor subtypes, SX-3228 preferentially binds to the BZ1 receptor with IC50 of 17 nM. It has very weak affinity for the BZ2 receptor (spinal cord: IC50=127 nM), and virtually no affinity for the peripheral type BZ receptor (kidney: IC50>10000 nM). SX-3228 has been shown to bind to BZ receptors, but not to dopamine (D1, D2), serotonin (5-HT1, 5-HT2 and 5-HT3 subtypes), noradrenaline (α1, α2, β), GABA or acetylcholine (muscarinic) subtypes. |
In vivo | Administering SX-3228 at doses ranging from 0.5 to 2.5 mg/kg to rats during their active (light) phase significantly diminishes rapid-eye-movement sleep (REMS) (P<0.05), particularly in the third hour of observation. Conversely, introducing SX-3228 in the same dosage range at the onset of the inactive (dark) phase profoundly alters sleep architecture: it markedly reduces wakefulness (W) and enhances slow-wave sleep (SWS) throughout a 6-hour examination period in a dose-dependent manner (P<0.05-0.01). Notably, these significant effects in the final hour are exclusively observed at the highest administered dose of 2.5 mg/kg (P<0.01). |
Molecular Weight | 338.36 |
Formula | C18H18N4O3 |
CAS No. | 156364-04-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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SX-3228 156364-04-4 Others SX 3228 SX3228 inhibitor inhibit