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Enerisant HCl is a novel potent and selective histamine H3 receptor antagonist, a substrate for P-gp, mediated by cytochrome P450 (CYP) and transporter proteins.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $93 | In Stock | |
| 5 mg | $227 | In Stock | |
| 10 mg | $365 | In Stock | |
| 25 mg | $592 | In Stock | |
| 50 mg | $857 | In Stock | |
| 100 mg | $1,150 | In Stock |
| Description | Enerisant HCl is a novel potent and selective histamine H3 receptor antagonist, a substrate for P-gp, mediated by cytochrome P450 (CYP) and transporter proteins. |
| In vivo | Enerisant HCl (0.3-1 mg/kg; p.o.; once; Male SD rats) attenuates the biphagous response in rats.[1] Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once; Male SD rats) causes histamine H3 receptor occupancy in a dose-dependent manner in rats. The dose causing half-maximal receptor occupancy was 0.78 mg/kg.[1] Enerisant HCl (1 mg/kg; s.c.; once; Male SD rats) increases total extracellular histamine levels in the posterior hypothalamus of rats.[1] Enerisant HCl (1 mg/kg; i.p.; once; Male SD rats) increases total extracellular dopamine and acetylcholine levels in the rat medial prefrontal cortex (mPFC).[1] |
| Molecular Weight | 434.96 |
| Formula | C22H31ClN4O3 |
| Cas No. | 1152749-07-9 |
| Smiles | C(=O)(C1=CN(N=C1)C2=CC=C(OCCCN3[C@H](C)CCC3)C=C2)N4CCOCC4.Cl |
| Color | White |
| Appearance | Oil |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (114.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.6 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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