Enerisant
CAS No. : 1152747-82-4
(Synonyms: TS-091)
| Size | Price | Stock |
|---|---|---|
| 5mg | $220 | In-stock |
| 10mg | $360 | In-stock |
| 25mg | $760 | In-stock |
| 50mg | $980 | In-stock |
| 100mg | $1380 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-17610 |
| M.Wt: | 398.50 |
| Formula: | C22H30N4O3 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
Enerisant (TS-091) is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively[1].
IC50 & Target:IC50: 2.89 nM (human histamine H3 receptor), 14.5 nM (rat histamine H3 receptor)
Ki: 1.65 nM (human histamine H3 receptor), 7.87 nM (rat histamine H3 receptor)[1]
In Vivo:Enerisant hydrochloride (0.3-1 mg/kg; p.o.; once) attenuats the dipsogenia response in rats[1].
Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once) results in the occupancy of the histamine H3 receptor in a dose-dependent manner in rats. A dose eliciting a half-maximal receptor occupancy is 0.78 mg/kg[1].
Enerisant hydrochloride (1 mg/kg; s.c.; once) increases the total extracellular histamine levels in the posterior hypothalamus in rats[1].
Enerisant hydrochloride (1 mg/kg; i.p.; once) increases the total extracellular dopamine and acetylcholine levels in the medial prefrontal cortex (mPFC) in rats[1].
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