| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
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| Targets |
Imetit Dihydrobromide primarily targets the histamine H3 and H4 receptors, both of which are G-protein-coupled receptors (GPCRs). It exhibits extremely high affinity for these targets, with reported Ki values of 0.3 nM for the H3 receptor and 2.7 nM for the H4 receptor. The H3 receptor is predominantly expressed in the central nervous system where it modulates the release of various neurotransmitters, while the H4 receptor is mainly found on peripheral immune cells, playing a key role in inflammatory responses and chemotaxis.
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| ln Vitro |
In vitro, Imetit Dihydrobromide demonstrates potent functional activity at the histamine H4 receptor. It effectively mimics the effect of histamine on eosinophil shape change, a process indicative of cytoskeletal rearrangement and cell activation, with an EC50 value of 25 nM. This activity highlights its role in mediating immune cell functions. Additionally, its action at the H3 receptor is well-characterized, where it is considered equipotent or slightly more active than the standard H3 agonist (R)-α-methylhistamine.
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| ln Vivo |
Imetetide dihydrobromide (2.5-10 mg/kg; intraperitoneally) decreases apomorphine-induced licking reflexes [4].
In vivo, Imetit Dihydrobromide is used to explore the physiological and pathophysiological roles of histamine H3 and H4 receptors. In animal models, administration of Imetit (2.5-10 mg/kg, i.p.) has been shown to reduce apomorphine-induced licking behavior in rats, demonstrating its modulatory effects on dopaminergic and histaminergic pathways in the central nervous system. These studies are instrumental in understanding the H3 receptor's role in motor control and neurological disorders. Its activity at the H4 receptor is also studied in models of inflammation and allergic responses. |
| Enzyme Assay |
The binding affinity of Imetit Dihydrobromide for H3 and H4 receptors is typically determined using radioligand binding assays. Membrane preparations from cells expressing the recombinant receptors are incubated with varying concentrations of the compound and a radiolabeled antagonist, such as [³H]-N-methylhistamine for the H3 receptor. Nonspecific binding is determined in the presence of an excess of unlabeled ligand, and the Ki values are calculated from competitive binding curves.
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| Cell Assay |
To assess the functional activity of Imetit Dihydrobromide at the H4 receptor, isolated eosinophils are treated with increasing concentrations of the compound. The shape change response, which indicates cytoskeletal rearrangement and cell activation, is quantified using flow cytometry. The EC50 for this shape change, reported at 25 nM, is a standard measure of the compound's functional potency.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [4]
Doses: 2.5, 5, 10 mg/kg Route of Administration: intraperitoneal (ip) injection (30 minutes before apomorphine) Experimental Results: diminished apomorphine-induced licking response. In animal studies, Imetit Dihydrobromide is typically administered via intraperitoneal (i.p.) injection to evaluate its effects on histamine receptor-mediated responses. In a typical protocol, male Sprague-Dawley rats are treated with the compound at doses of 2.5, 5, or 10 mg/kg, 30 minutes prior to the administration of apomorphine. The reduction in apomorphine-induced licking behavior is then measured to assess the compound's modulatory effects on central dopaminergic pathways. |
| ADME/Pharmacokinetics |
As a dihydrobromide salt, Imetit Dihydrobromide exhibits good aqueous solubility, which facilitates its administration and absorption in biological systems. As a small molecule agonist, it is expected to have a moderate half-life and to distribute to tissues expressing H3 and H4 receptors, including the brain (for H3) and peripheral immune cells (for H4). Its pharmacokinetic profile is suitable for use as a research tool in both in vitro and in vivo settings.
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| Toxicity/Toxicokinetics |
As a potent receptor agonist, Imetit Dihydrobromide may cause adverse effects related to excessive histamine receptor activation. These could include modulation of gastric acid secretion, central nervous system effects such as alterations in sleep-wake regulation, and modulation of immune responses. In animal models, high doses may potentiate the effects of other compounds acting on the histaminergic system.
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| References |
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| Additional Infomation |
Imetit dihydrobromide is a hydrobromide salt prepared by reacting imetate with two equivalents of hydrobromic acid. It is a potent and highly affinity agonist for both H3 and H4 receptors (Ki values of 0.3 nM and 2.7 nM, respectively). It induces morphological changes in eosinophils, with an EC50 value of 25 nM. After systemic administration, it is active in the central nervous system. It is an agonist of both H4 and H3 receptors. It contains one imetate(2+) ion.
Imetit Dihydrobromide has been widely employed as a reference compound in preclinical research to validate novel histamine receptor ligands. It is not approved for clinical use and serves primarily as a research tool to dissect H3 and H4 receptor pharmacology in neurological and immunological contexts. Key studies have utilized it to investigate the role of histamine receptors in conditions such as experimental allergic rhinitis, obesity, and alcohol-induced sedation. |
| Molecular Formula |
C6H10N4S.2[HBR]
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|---|---|
| Molecular Weight |
332.05928
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| Exact Mass |
329.915
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| CAS # |
32385-58-3
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| PubChem CID |
11957573
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| Appearance |
White to light brown solid powder
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| Boiling Point |
430.8ºC at 760mmHg
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| Melting Point |
206 - 207 °C
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| Flash Point |
214.3ºC
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| LogP |
3.295
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
139
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DOBOYMKCRRLTRF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H10N4S.2BrH/c7-6(8)11-2-1-5-3-9-4-10-5;;/h3-4H,1-2H2,(H3,7,8)(H,9,10);2*1H
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| Chemical Name |
2-(1H-imidazol-5-yl)ethyl carbamimidothioate;dihydrobromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 3.0115 mL | 15.0575 mL | 30.1150 mL | |
| 5 mM | 0.6023 mL | 3.0115 mL | 6.0230 mL | |
| 10 mM | 0.3012 mL | 1.5058 mL | 3.0115 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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