Art. -Nr.: HY-10559

Nelotanserin

(Synonyms: APD125)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Nelotanserin is a potent 5-HT_2A inverse agonist, a moderately potent 5-HT_2C partial inverse agonist and a weak 5-HT_2B inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

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Reinheit: 99.66%
CAS. Nr.: 839713-36-9
Formel: C₁₈H₁₅BrF₂N₄O₂
Molecular Weight:437.24

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nelotanserin Chemical Structure

CAS. Nr.: 839713-36-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

5-HT_2A Receptor

1.7 nM (IC₅₀)

5-HT_2C Receptor

79 nM (IC₅₀)

5-HT_2B Receptor

791 nM (IC₅₀)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT_2A full inverse agonist (IC₅₀=1.7 nM), a moderately potent 5-HT_2C partial inverse agonist (IC₅₀=79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a weak 5-HT_2B inverse agonist (IC₅₀=791 nM). Nelotanserin displays high affinity for recombinant human 5-HT_2A receptors (K_i=0.35 nM), moderate affinity for human 5-HT_2C receptors (K_i=100 nM), and low affinity for human 5-HT_2B receptors (2000 nM) stably expressed in HEK293 cells. The results suggest that Nelotanserin has a 262-fold higher affinity for human 5-HT_2A than 5-HT_2C receptors and a 6610-fold higher affinity for human 5-HT_2A than 5-HT_2B receptors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Each compound is tested in a minimum of five rats by oral gavage with administration occurring in the middle of the inactive period, 6 h after light onset. The delta power during non-REM sleep (NREMS) is significantly different between all the analogues tested and the vehicle control. Nelotanserin (Compound 39) produces significant increases in delta power that persist for the first 4 h following dosing. Significant differences are found, however, in NREMS bout length. Nelotanserin significantly increases NREMS bout length during the first hour following dosing, and 3 does so during the second hour. In conjunction with this increased NREM bout duration, the number of NREM bouts decrease during the first hour for Nelotanserin (p<0.01) as well as for compound 15 (p<0.05)^[2].

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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 839713-36-9
Appearance Solid
Molecular Weight 437.24
Formel C₁₈H₁₅BrF₂N₄O₂
Color White to off-white
SMILES

COC1=C(C2=C(Br)C=NN2C)C=C(NC(NC3=C(F)C=C(F)C=C3)=O)C=C1
Synonyms

APD125
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

ACS Chem Neurosci

Big Data Challenges Targeting Proteins in GPCR Signaling Pathways; Combining PTML-ChEMBL Models and [35S]GTPγS Binding Assays. [Abstract]

2019 Nov 20;10(11):4476-4491. PMID: 31618004
Behav Brain Res

Nelotanserin, a selective 5-HT2A receptor inverse agonist, attenuates aspects of nicotine withdrawal but not reward in mice. [Abstract]

2024 Jun 5:467:115019. PMID: 38677331

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 32 mg/mL (73.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2871 mL

11.4354 mL

22.8707 mL

5 mM

0.4574 mL

2.2871 mL

4.5741 mL

10 mM

0.2287 mL

1.1435 mL

2.2871 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Al-Shamma HA et al. Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia. J Pharmacol Exp Ther. 2010 Jan;332(1):281-90. [Content Brief]

[2]. Teegarden BR et al. Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia. J Med Chem. 2010 Mar 11;53(5):1923-36. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2871 mL	11.4354 mL	22.8707 mL	57.1768 mL
	5 mM	0.4574 mL	2.2871 mL	4.5741 mL	11.4354 mL
	10 mM	0.2287 mL	1.1435 mL	2.2871 mL	5.7177 mL
	15 mM	0.1525 mL	0.7624 mL	1.5247 mL	3.8118 mL
	20 mM	0.1144 mL	0.5718 mL	1.1435 mL	2.8588 mL
	25 mM	0.0915 mL	0.4574 mL	0.9148 mL	2.2871 mL
	30 mM	0.0762 mL	0.3812 mL	0.7624 mL	1.9059 mL
	40 mM	0.0572 mL	0.2859 mL	0.5718 mL	1.4294 mL
	50 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1435 mL
	60 mM	0.0381 mL	0.1906 mL	0.3812 mL	0.9529 mL

Keywords

Nelotanserin

2 Cited Publications

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Nelotanserin

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Publications Citing Use of MedChemExpress (MCE) Nelotanserin

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nelotanserin

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

5-HT Receptor Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Nelotanserin

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nelotanserin Related Classifications

HY-10559 Related Classifications