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Naluzotan hydrochloride

Catalog No. T68113 CAS 740873-82-9

Synonyms: PRX 00023 hydrochloride

Naluzotan hydrochloride (PRX 00023 hydrochloride) is a hERG K+ channel blocker with an IC50 value of 3800 nM and is commonly used in the study of anxiety and depression.Naluzotan hydrochloride is also a novel, potent, and selective 5-HT1A agonist, with an IC50 value of about 20 nM and a Ki value of about 5.1 Naluzotan hydrochloride is also a novel, potent and selective 5-HT1A agonist with an IC50 of approximately 20 nM and a Ki of approximately 5.1 nM.

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Naluzotan hydrochloride Chemical Structure

Naluzotan hydrochloride, CAS 740873-82-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 230.00
5 mg	In stock	$ 570.00
10 mg	In stock	$ 817.00
25 mg	In stock	$ 1,250.00
50 mg	In stock	$ 1,680.00
100 mg	In stock	$ 2,270.00
500 mg	In stock	$ 4,550.00

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Purity: 98.61%

Biological Description

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Description	Naluzotan hydrochloride (PRX 00023 hydrochloride) is a hERG K+ channel blocker with an IC50 value of 3800 nM and is commonly used in the study of anxiety and depression.Naluzotan hydrochloride is also a novel, potent, and selective 5-HT1A agonist, with an IC50 value of about 20 nM and a Ki value of about 5.1 Naluzotan hydrochloride is also a novel, potent and selective 5-HT1A agonist with an IC50 of approximately 20 nM and a Ki of approximately 5.1 nM.
Targets&IC50	5-HT1A:20 nM, 5-HT1A:5.1 nM, ERG K+ (human):3800 nM
In vitro	Naluzotan hydrochloride behaves as a full agonist in an in vitro cell-based functional assay with an EC50 of 20 nM. Naluzotan hydrochloride has significant affinity is the guinea pig sigma receptor (Ki = 100 nM), but does not inhibit cytochrome P450 isoforms (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4.[1]
In vivo	In rats Naluzotan hydrochloride shows 11% oral bioavailability with a serum t1/2 of 2−3.5 h when administrated po, attaining a Cmax level of 24 ± 13 ng/mL (3 mg/kg, po). Naluzotan hydrochloride shows significant brain penetration, achieving a brain:serum concentration ratio of approximately 0.5 in the rat at 1 h following either intravenous or oral administration and reaching brain concentration approximately equivalent to that of buspirone. In dogs the pharmacokinetic profile of Naluzotan hydrochloride shows 16% oral bioavailability, a serum t1/2 of 1.1 h po, and a Cmax level of 174 ± 141 ng/mL (3 mg/kg, po)[1]. PRX-00023 (0.01-0.05 mg/kg, i.p.) significantly reduces USV rates, but done of these doses produce sedation in rats.[2]

Synonyms	PRX 00023 hydrochloride
Molecular Weight	487.1
Formula	C23H39ClN4O3S
CAS No.	740873-82-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Becker OM, et al. An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. J Med Chem. 2006 Jun 1;49(11):3116-35. 2. Brunelli SA, et al. PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety. Pharmacol Biochem Behav. 2009 Nov;94(1):8-15.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library

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Keywords

Naluzotan hydrochloride 740873-82-9 Angiogenesis GPCR/G Protein JAK/STAT signaling Neuroscience Tyrosine Kinase/Adaptors EGFR 5-HT Receptor PRX 00023 hydrochloride Naluzotan Hydrochloride PRX 00023 Hydrochloride PRX00023 Hydrochloride PRX-00023 Hydrochloride inhibitor inhibit

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