store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 700.00 | |
5 mg | In stock | $ 1,800.00 |
Description | Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression. |
Targets&IC50 | Cell-based functional assay:20 nM (EC50), 5-HT1A receptor:20 nM, 5-HT1A receptor:5.1 nM (Ki), σ receptor:100 nM (Ki,guinea pig), ERG K+ channel (human):3800 nM |
In vitro | Naluzotan, with an EC50 of 20 nM, behaves as a full agonist in an in vitro cell-based functional assay. It exhibits significant affinity for the guinea pig sigma receptor (Ki = 100 nM) but does not inhibit cytochrome P450 isoforms (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4[2]. |
In vivo | In rats, when administered orally, Naluzotan shows 11% oral bioavailability with a serum half-life (t1/2) of 2−3.5 hours, reaching a Cmax level of 24 ± 13 ng/mL (3 mg/kg, oral). Naluzotan exhibits significant brain penetration, with a brain:serum concentration ratio of approximately 0.5 in rats at 1 hour following either intravenous or oral administration, and it achieves a brain concentration approximately equivalent to that of buspirone. In dogs, the pharmacokinetic profile of naluzotan demonstrates 16% oral bioavailability, a serum t1/2 of 1.1 hours when administered orally, and a Cmax level of 174 ± 141 ng/mL (3 mg/kg, oral)[1]. PRX-00023, at doses of 0.01-0.05 mg/kg administered intraperitoneally, significantly reduces ultrasonic vocalization (USV) rates in rats, but none of these doses induce sedation[1]. |
Synonyms | PRX 00023 |
Molecular Weight | 450.64 |
Formula | C23H38N4O3S |
CAS No. | 740873-06-7 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Naluzotan 740873-06-7 Angiogenesis GPCR/G Protein JAK/STAT signaling Neuroscience Tyrosine Kinase/Adaptors EGFR 5-HT Receptor PRX 00023 PRX00023 PRX-00023 inhibitor inhibit