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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.05%
- CAS. Nr.: 740873-06-7
- Formel: C23H38N4O3S
- Molecular Weight:450.64
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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5-HT1A Receptor |
5-HT1A Receptor 20 nM (IC50) |
5-HT1A Receptor 5.1 nM (Ki) |
hERG K+ channel 3800 nM (IC50) |
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Cell Line
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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
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[PMID: 16722631] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 740873-06-7
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Appearance Solid
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Molecular Weight 450.64
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protokoll
PRX-00023 and buspirone are used in the assay. Drugs are dissolved in saline vehicle prior to injections. Each pup is injected in the intraperitoneal space (i.p.) with one of several doses of PRX-00023 (0.01, 0.03, 0.05, 0.1, 0.3, 1.0, and 3.0 mg/kg in saline, for a total volume of 0.1 mg/kg). Within each litter two littermates, though occasionally one, receive the same dose of a compound. Because of the distribution of pups in litters used, no Random line pups are tested with PRX-00023 at 3.0 mg/kg for comparison to vehicle.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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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)
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Naluzotan Related Classifications
HY-14848 Related Classifications
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