Naluzotan
Based on 1 Customer Validation
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
For research use only. We do not sell to patients.
- Purity : 98.05%
- CAS No.: 740873-06-7
- Formula: C23H38N4O3S
- Molecular Weight:450.64
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
|
5-HT1A Receptor |
5-HT1A Receptor 20 nM (IC50) |
5-HT1A Receptor 5.1 nM (Ki) |
hERG K+ channel 3800 nM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
3800 nM
Compound: 20m
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Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay
Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay
|
[PMID: 16722631] |
In Vitro
Naluzotan behaves as a full agonist in an in vitro cell-based functional assay with an EC50 of 20 nM. Naluzotan 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 740873-06-7
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Appearance Solid
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Molecular Weight 450.64
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Formula C23H38N4O3S
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Color White to light yellow
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SMILES
CC(NC1=CC=CC(N2CCN(CCCCNS(=O)(CC3CCCCC3)=O)CC2)=C1)=O
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Synonyms
PRX 00023
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)