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Samelisant

Catalog No. T9770 CAS 1394808-82-2

Synonyms: SUVN-G3031

Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

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Samelisant, CAS 1394808-82-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 113.00
2 mg	In stock	$ 169.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 463.00
25 mg	In stock	$ 763.00
50 mg	In stock	$ 1,070.00
100 mg	In stock	$ 1,430.00
500 mg	In stock	$ 2,890.00
1 mL * 10 mM (in DMSO)	In stock	$ 297.00

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Purity: 99.09%

Biological Description

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Storage & Solubility Information

Description	Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.
In vitro	Samelisant (1, 10, and 100 nM) increases the pEC50 from 8.5 to 8.2, 7.3, and 6.2 for human H3 receptor and from 8.2 to 7.9, 7.4, and 6.4 for rat H3 receptor, respectively. Samelisant modulates dopamine and norepinephrine levels in the cerebral cortex. Samelisant reversibly binds to the orthosteric site with Kbs of 1.3 nM and 1.1 nM[1].
In vivo	In orexin knockout mice subjected to sleep EEG, Samelisant (10 and 30 mg/kg; p.o.) significantly increases wakefulness and concomitantly decreases NREM sleep. Samelisant significantly decreases direct REM sleep onset episodes and dose-dependently increases the level of tele-methylhistamine[1].

Synonyms	SUVN-G3031
Molecular Weight	373.49
Formula	C21H31N3O3
CAS No.	1394808-82-2

Storage

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

Solubility Information

DMSO: 50 mg/mL (112.01 mM), Sonication and heating to 60℃ are recommended.

References and Literature

1. Nirogi R, et al. Samelisant (SUVN-G3031), a potent, selective and orally active histamine H3 receptor inverse agonist for the potential treatment of narcolepsy: pharmacological and neurochemical characterisation. Psychopharmacology (Berl). 2021 Jun;238(6):1495-1511.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library

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Keywords

Samelisant 1394808-82-2 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor SUVN-G3031 SUVN-G 3031 SUVN-G-3031 inhibitor inhibit

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