| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Histamine H1 receptor (potent, selective, long-acting antagonist). It has much lower affinity for H2 receptors, α- and β-adrenergic receptors, serotonin, and muscarinic receptor subtypes.
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|---|---|
| ln Vitro |
In vitro radioligand binding tests reveal that tazafilinolone has a high affinity for histamine H1 receptors, which in turn potently suppresses contractions caused by activation of these receptors in the isolated guinea pig ileum. Tazifylline's affinity for alpha and beta adrenergic receptors, histamine H2 receptors, and 5-adrenergic receptors is significantly reduced. Subtypes of muscarinic and serotonin receptors. Rat peritoneal mast cells' ability to release histamine is poorly inhibited by tacicoline [1].
In vitro, (±)-Tazifylline potently antagonizes histamine H1 receptor-mediated responses. It is selective for the H1 receptor with significantly lower affinity for other receptor types including H2, adrenergic, serotonin, and muscarinic receptors. Quantitative IC50 or Ki values are not detailed in publicly available sources. |
| ln Vivo |
In rats, guinea pigs, and dogs, tazicoline has antihistamine effects that start quickly and last a long time. Tazicoline effectively prevented histamine-induced bronchoconstriction in anesthetized guinea pigs and shielded conscious animals from the deadly consequences of high amine dosages. Tazicoline is more effective than intradermal histamine inflammatory effects generated by anaphylaxis in awake rats. Tazicoline taken orally reduces histamine-induced skin inflammation in dogs that are awake and lessens histamine-induced hypotension in animals that are sedated because it stimulates H1 receptors. Oral treatment of statizine at high doses does not cause substantial behavioral indications of depression in awake rats or decrease spontaneous locomotor activity in mice [1].
In vivo, (±)-Tazifylline is a long-acting H1 receptor antagonist. It has been studied for its potential in treating allergic conditions. Detailed dose-response and pharmacokinetic data in animal models are limited in publicly available literature. |
| Enzyme Assay |
No specific cell-free H1 receptor binding assay protocol is detailed for Tazifylline. For H1 receptor antagonists, typical cell-free assays include radioligand binding studies using [3H]mepyramine or [3H]pyrilamine and membrane preparations from tissues expressing H1 receptors.
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| Cell Assay |
Cellular H1 receptor antagonism is assessed in cells expressing H1 receptors (e.g., histamine-induced calcium flux assays). Cells are treated with Tazifylline and stimulated with histamine; inhibition of the response is measured. Selectivity can be confirmed by testing against other receptor types.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of allergy (e.g., histamine-induced skin wheal, ovalbumin-induced allergic rhinitis). Tazifylline is administered via oral or intravenous routes. Endpoints include symptom scores, histamine challenge response, and inflammatory biomarker analysis.
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| ADME/Pharmacokinetics |
Molecular weight: 472.60 g/mol; molecular formula: C23H32N6O3S. CAS No.: 79712-55-3. IUPAC name: 7-(2-hydroxy-3-(4-(3-(phenylthio)propyl)piperazin-1-yl)propyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione. Storage: typical for small-molecule compounds (desiccated, protected from light).
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a histamine H1 receptor antagonist, potential side effects may include sedation, dry mouth, and other antihistamine-related effects at high doses. Standard toxicological studies would be required for drug development.
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| References |
[1]. Poizot A, et al. Animal pharmacology of the selective histamine H1-receptor antagonist tazifylline. Arzneimittelforschung. 1986 Apr;36(4):695-702.
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| Additional Infomation |
(±)-Tazifylline is a research-grade compound, not approved for therapeutic use. It is primarily used as a pharmacological tool for studying histamine H1 receptor function and allergic responses. No clinical trials have been reported. Its mechanism involves selective H1 receptor antagonism.
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| Molecular Formula |
C23H32N6O3S
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|---|---|
| Molecular Weight |
472.60358
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| Exact Mass |
472.226
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| CAS # |
79712-55-3
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| Related CAS # |
79712-53-1 (dihydrochloride)
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| PubChem CID |
54424
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.34g/cm3
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| Boiling Point |
705.1ºC at 760 mmHg
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| Flash Point |
380.2ºC
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| Index of Refraction |
1.668
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| LogP |
0.47
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
671
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C)C(=O)N(C)C2N=CN(C1=2)CC(CN1CCN(CCCSC2C=CC=CC=2)CC1)O
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| InChi Key |
JTOUASWUIMAMAD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H32N6O3S/c1-25-21-20(22(31)26(2)23(25)32)29(17-24-21)16-18(30)15-28-12-10-27(11-13-28)9-6-14-33-19-7-4-3-5-8-19/h3-5,7-8,17-18,30H,6,9-16H2,1-2H3
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| Chemical Name |
7-[2-hydroxy-3-[4-(3-phenylsulfanylpropyl)piperazin-1-yl]propyl]-1,3-dimethylpurine-2,6-dione
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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 | 2.1160 mL | 10.5798 mL | 21.1595 mL | |
| 5 mM | 0.4232 mL | 2.1160 mL | 4.2319 mL | |
| 10 mM | 0.2116 mL | 1.0580 mL | 2.1160 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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