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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $113 | In Stock | |
2 mg | $169 | In Stock | |
5 mg | $289 | In Stock | |
10 mg | $463 | In Stock | |
25 mg | $763 | In Stock | |
50 mg | $1,070 | In Stock | |
100 mg | $1,430 | In Stock | |
500 mg | $2,890 | In Stock | |
1 mL x 10 mM (in DMSO) | $297 | In Stock |
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]. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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