| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Bamirastine targets the histamine H1 receptor, a G protein-coupled receptor that mediates the effects of histamine in allergic and inflammatory responses. Histamine H1 receptors are widely expressed in various tissues, including smooth muscle, endothelium, and the central nervous system. Activation of H1 receptors by histamine leads to vasodilation, increased vascular permeability, smooth muscle contraction, and pruritus (itching). Bamirastine inhibits ligand binding to the recombinant human H1 receptor with an IC50 of 17.3 nM. By blocking H1 receptor activation, Bamirastine suppresses histamine-mediated allergic responses. The compound is also known as TAK-427.
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| ln Vitro |
Bamirastine (TAK-427) has an IC50 value of 17.3 nM and decreases the concentration-dependent specific binding of [3H]pyrilamine to recombinant human H1 receptor (rhH1R). A value of 7.35 nM was determined for the Ki. Based on research, bamistin's affinity is 3 times higher than fenadine, 2 times lower than epinastine, 8 times lower than ketotifen, and as high as azelastine [1].
Bamirastine demonstrates potent in vitro activity as an H1 receptor antagonist with an IC50 of 17.3 nM in ligand binding assays. The compound effectively inhibits the binding of histamine to the recombinant human H1 receptor. In cellular assays, Bamirastine blocks H1 receptor-mediated signaling, including calcium mobilization and other downstream effects. The compound has been shown to inhibit allergic skin inflammation, consistent with its H1 receptor antagonist activity. Bamirastine's potent and selective H1 receptor antagonism makes it a valuable tool for studying histamine signaling and allergic inflammatory responses. |
| ln Vivo |
In guinea pigs and mice, bamirastine (TAK-427) inhibits histamine-induced skin reactions with ID50 values of 0.884 and 0.450 mg/kg, respectively, when administered orally; 24 hours after dosing, in guinea pigs, the same effects as 10 mg/kg Bamirastine were still observed in guinea pigs Stine-related significant inhibition. In mice, even at 300 mg/kg, bamistin had no effect on the length of pentobarbital-induced drowsiness. Bamistin clearly suppresses antigen-induced immunological response (ISR) in guinea pigs and mice, as well as the passive cutaneous allergic response (PCA) in mice [1].
Bamirastine has been evaluated in vivo for its ability to inhibit allergic responses. The compound inhibits allergic skin inflammation, demonstrating its efficacy in a relevant in vivo model of allergic disease. In preclinical studies, Bamirastine has been administered orally at doses of 30, 100, and 300 mg/kg. The compound's effects on allergic inflammation have been characterized in these models. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature. Bamirastine is a valuable tool for studying the role of H1 receptors in allergic diseases and for evaluating H1 receptor antagonists as therapeutic agents. |
| Enzyme Assay |
The in vitro receptor binding assay for Bamirastine measures the inhibition of ligand binding to the recombinant human histamine H1 receptor. Membrane preparations from cells expressing the recombinant human H1 receptor are incubated with varying concentrations of Bamirastine (typically ranging from nanomolar to micromolar) in the presence of a radiolabeled H1 receptor ligand (e.g., 3H-mepyramine or 3H-pyrilamine). The amount of bound radioligand is measured by scintillation counting, and IC50 values are determined by fitting competition binding curves. The compound is dissolved in DMSO and diluted in assay buffer to achieve the desired final concentrations, with DMSO concentration kept constant across all wells. Appropriate positive controls (known H1 receptor antagonists) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
The in vitro cellular assay for Bamirastine is performed using cells expressing the human H1 receptor, such as CHO or HEK293 cells stably transfected with H1R. Cells are cultured in appropriate medium and loaded with a calcium-sensitive fluorescent dye. Cells are treated with varying concentrations of Bamirastine or vehicle control (DMSO) prior to stimulation with histamine. The increase in intracellular calcium is measured using a fluorescence plate reader. The inhibition of histamine-induced calcium mobilization by Bamirastine is quantified, and IC50 values are determined by fitting dose-response curves. Alternatively, the compound's effects on H1 receptor-mediated signaling can be assessed by measuring inositol phosphate accumulation or other downstream signaling events. The compound's selectivity for H1 over other histamine receptors can also be assessed.
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| Animal Protocol |
In vivo animal experiments with Bamirastine are typically conducted using models of allergic inflammation, such as passive cutaneous anaphylaxis or contact hypersensitivity models. Bamirastine is administered orally at various doses (e.g., 30, 100, and 300 mg/kg). Allergic responses are induced by appropriate sensitization and challenge protocols. The extent of allergic inflammation (e.g., skin edema, inflammatory cell infiltration, or cytokine production) is measured and compared to vehicle-treated controls. The compound's ability to inhibit allergic inflammation is quantified. Behavior is observed for the first 2 hours after drug administration to assess any central nervous system effects. Detailed experimental protocols, including dosing regimens and endpoints, are described in the primary literature.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for Bamirastine are not extensively documented in publicly available sources. As a small-molecule H1 receptor antagonist with a molecular weight of 527.66, the compound is expected to have reasonable oral bioavailability. Bamirastine has a chemical formula of C31H37N5O3. The compound is soluble in DMSO for formulation purposes. For in vivo oral administration, Bamirastine is typically formulated using appropriate vehicles such as 0.5% methylcellulose to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Bamirastine are not extensively documented in publicly available sources. As a research-grade compound, Bamirastine is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. In animal studies, Bamirastine has been administered orally at doses up to 300 mg/kg with behavioral monitoring. However, comprehensive toxicological profiling (e.g., LD50, maximum tolerated dose, organ-specific toxicity) is not available from the current search results and would require consultation of the primary literature or safety data sheets.
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| References | |
| Additional Infomation |
Bamirastine is a research compound developed for studying histamine H1 receptor signaling and allergic inflammatory responses. The compound inhibits ligand binding to the recombinant human H1 receptor with an IC50 of 17.3 nM. Bamirastine has been shown to inhibit allergic skin inflammation. The compound is also known as TAK-427. Bamirastine is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical research. The compound is available from various chemical suppliers for research purposes. Its utility lies in its ability to selectively inhibit H1 receptors and probe their role in allergic and inflammatory responses.
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| Molecular Formula |
C31H37N5O3
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| Molecular Weight |
527.6572
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| Exact Mass |
527.29
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| CAS # |
215529-47-8
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| PubChem CID |
9806921
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.523
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
39
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| Complexity |
743
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])N([H])C2C([H])=C([H])C3=NC(=C([H])N3N=2)C(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])C1([H])[H]
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| InChi Key |
WTBRUSNNZKWTMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H37N5O3/c1-31(2,30(37)38)26-22-36-28(33-26)15-14-27(34-36)32-18-9-19-35-20-16-25(17-21-35)39-29(23-10-5-3-6-11-23)24-12-7-4-8-13-24/h3-8,10-15,22,25,29H,9,16-21H2,1-2H3,(H,32,34)(H,37,38)
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| Chemical Name |
2-[6-[3-(4-benzhydryloxypiperidin-1-yl)propylamino]imidazo[1,2-b]pyridazin-2-yl]-2-methylpropanoic acid
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| Synonyms |
TAK-427; TAK 427; TAK427
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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 | 1.8952 mL | 9.4758 mL | 18.9516 mL | |
| 5 mM | 0.3790 mL | 1.8952 mL | 3.7903 mL | |
| 10 mM | 0.1895 mL | 0.9476 mL | 1.8952 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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