10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Panoramica
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 IC 50 s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
In Vitro
Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT 2A full inverse agonist (IC 50 =1.7 nM), a moderately potent 5-HT 2C partial inverse agonist (IC 50 =79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a weak 5-HT 2B inverse agonist (IC 50 =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. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC 50 s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
Condizioni di conservazione di stoccaggio
Store at -80°C
Spedito in
Dry ice packs + Cold packs
Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.
Certificati (CoA, COO, BSE/TSE e tabella di analisi)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
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Recensioni
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Domande frequenti
How should this product be stored?
Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.
How is this product shipped?
This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 839713-36-9, the molecular formula is C18H15BrF2N4O2, and the molecular weight is 437.24 g/mol.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
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