| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Enerisant selectively targets the histamine H3 receptor, a presynaptic autoreceptor that regulates the release of histamine and other neurotransmitters in the brain. It acts as a potent antagonist/inverse agonist with IC₅₀ values of 2.89 nM for the human histamine H3 receptor and 14.5 nM for the rat histamine H3 receptor. By blocking the H3 receptor, enerisant enhances histaminergic neurotransmission, which is believed to improve cognitive function.
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| ln Vitro |
In vitro, enerisant is a potent and highly selective histamine H3 receptor antagonist/inverse agonist with IC₅₀ values of 2.89 nM (human) and 14.5 nM (rat). It is a competitive inhibitor, suggesting it binds to the same site as the endogenous ligand, histamine. Its high selectivity for the H3 receptor over other histamine receptor subtypes contributes to its targeted mechanism of action and potential for a favorable side effect profile.
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| ln Vivo |
Enerisant hydrochloride (0.3–1 mg/kg; po; once) Amphiphilic reactions that are dependent on cosmetics [1]. The posterior hypothalamus's total extracellular histamine levels are raised by enerisant hydrochloride (1 mg/kg; sc; once) [1]. In the thoracic medial prefrontal cortex (mPFC), enerisant hydrochloride (1 mg/kg; ip; Once) raises levels of bone choline and total extracellular dopamine [1].
In vivo, enerisant has been shown to modulate the histamine H3 receptor in a dose-dependent manner in mice. It promotes pro-cognitive effects and can reverse scopolamine-induced cognitive impairment in animal models. Its oral activity makes it a convenient candidate for in vivo studies of cognitive enhancement and other central nervous system applications. |
| Enzyme Assay |
Non-cellular receptor binding assays for enerisant involve competitive radioligand binding displacement studies using membrane preparations from cells expressing the human or rat histamine H3 receptor. Membranes are incubated with a radiolabeled H3 receptor ligand (e.g., [³H]-N-α-methylhistamine) and varying concentrations of enerisant. Following incubation and filtration, bound radioactivity is measured by scintillation counting. IC₅₀ values are determined from displacement curves and converted to Ki values.
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| Cell Assay |
In vitro cellular assays for enerisant involve treating cells expressing the histamine H3 receptor with the compound and measuring receptor-mediated signaling. Functional assays typically measure the inhibition of forskolin-stimulated cAMP accumulation, as H3 receptors are coupled to Gi proteins. Cells are treated with varying concentrations of enerisant and stimulated with a histamine H3 receptor agonist. The decrease in cAMP levels is quantified, and the IC₅₀ for antagonism is determined.
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| Animal Protocol |
Animal/Disease Models: Male SD rat, R-α-methylhistamine induction]. Dipsogenia Model[1]
Doses: 0.1, 0.3 and 1 mg/kg Route of Administration: po (po (oral gavage)) single dose Experimental Results: Attenuated Dipsogenia response, reaching statistical significance at doses of 0.3 mg/kg and 1 mg/kg. In vivo animal experiments with enerisant are conducted in rodent models of cognitive impairment. Scopolamine-treated rats or mice are used to model memory deficits, and enerisant is administered orally. Cognitive function is assessed using behavioral tests such as the object recognition test or the Morris water maze. The compound's ability to reverse scopolamine-induced cognitive impairment is evaluated. |
| ADME/Pharmacokinetics |
Enerisant has a molecular weight of 398.5 and a molecular formula of C₂₂H₃₀N₄O₃. It is a solid powder with a purity of ≥99.0%. The compound is soluble in DMSO (100 mg/mL). For storage, the powder should be kept at -20°C for up to 3 years or at 4°C for up to 2 years; stock solutions can be stored at -80°C for 6 months or at -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Enerisant is a research compound for laboratory use only and is not approved for human therapeutic use. In preclinical studies, it has been generally well-tolerated at therapeutic doses. As a histamine H3 receptor antagonist, it may cause side effects related to increased histaminergic tone, such as insomnia or gastrointestinal disturbances. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Enerisant (TS-091; CAS 1152747-82-4) is a potent, highly selective, competitive, and orally active histamine H3 receptor antagonist/inverse agonist. It has IC₅₀ values of 2.89 nM (human) and 14.5 nM (rat). Enerisant has demonstrated pro-cognitive effects and can reverse scopolamine-induced cognitive impairment. It has been investigated for the treatment of Alzheimer's disease and schizophrenia and is available from various commercial suppliers for research applications.
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| Molecular Formula |
C22H30N4O3
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|---|---|
| Molecular Weight |
398.498605251312
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| Exact Mass |
398.231
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| CAS # |
1152747-82-4
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| Related CAS # |
152749-07-9 (HCl);1152747-82-4;1152749-09-1 (HCl 2H2O);
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| PubChem CID |
42601503
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
586.2±50.0 °C at 760 mmHg
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| Flash Point |
308.3±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.620
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| LogP |
1.49
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
520
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H]1CCCN1CCCOC2=CC=C(C=C2)N3C=C(C=N3)C(=O)N4CCOCC4
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| InChi Key |
IABXVJILZYNSTM-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C22H30N4O3/c1-18-4-2-9-24(18)10-3-13-29-21-7-5-20(6-8-21)26-17-19(16-23-26)22(27)25-11-14-28-15-12-25/h5-8,16-18H,2-4,9-15H2,1H3/t18-/m1/s1
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| Chemical Name |
[1-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazol-4-yl]-morpholin-4-ylmethanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5094 mL | 12.5471 mL | 25.0941 mL | |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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