| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 1g | |||
| Other Sizes |
| Targets |
Thonzylamine hydrochloride acts as an antagonist at the H1 histamine receptor. By blocking the action of histamine at this receptor, it reduces allergic symptoms such as sneezing, itching, and runny nose. It also possesses anticholinergic properties, blocking the action of acetylcholine. It modulates Lamin A splicing with a potency of 35,481.3 nM and inhibits Tau fibril formation with a potency of 158.5 nM.
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|---|---|
| ln Vitro |
Thonzylamine hydrochloride inhibits the malarial parasite plastid with a potency of 10,691.0 nM and acts as an inhibitor of GCN5L2 at 39,810.7 nM. Its primary activity is as an H1 histamine receptor antagonist with good antihistaminic and antianaphylactic properties. Its anticholinergic properties contribute to its overall pharmacological profile.
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| ln Vivo |
In vivo studies of Thonzylamine hydrochloride have demonstrated its effectiveness in animal models of allergic disease, such as anaphylaxis. Its antihistaminic and antianaphylactic properties have been characterized in preclinical models. The compound's ability to cross the blood-brain barrier and its sedative effects are characteristic of first-generation antihistamines.
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| Enzyme Assay |
In vitro receptor binding assays for Thonzylamine hydrochloride measure its affinity for the H1 histamine receptor. The compound is incubated with membrane preparations expressing the H1 receptor and a radiolabeled ligand, and displacement is measured to determine binding affinity (Ki) values. Functional assays can assess its antagonist activity by measuring histamine-induced calcium mobilization or other downstream signaling events.
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| Cell Assay |
In vitro cellular assays for Thonzylamine hydrochloride involve treating cells expressing the H1 receptor with the compound to assess its antagonist activity. For example, histamine-induced calcium flux can be measured in the presence or absence of the compound. Its effects on cell viability and proliferation can also be assessed in various cell types. Antibacterial activity can be evaluated using standard susceptibility testing methods.
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| Animal Protocol |
In vivo animal models for Thonzylamine hydrochloride include the guinea pig model of anaphylaxis to assess its antianaphylactic properties. Other models, such as histamine-induced bronchoconstriction or skin wheal responses, are used to evaluate its antihistaminic activity. These models help determine the compound's efficacy and potency in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Thonzylamine hydrochloride are limited. As a first-generation antihistamine, it is expected to be well-absorbed after oral administration and to cross the blood-brain barrier, leading to sedative effects. It is metabolized in the liver, and its metabolites are excreted in urine. Its half-life and bioavailability are not well-characterized in the literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of Thonzylamine hydrochloride is similar to that of other first-generation antihistamines. Common side effects include sedation, drowsiness, dry mouth, and blurred vision due to its anticholinergic properties. It may cause dizziness and gastrointestinal disturbances. Overdose can lead to severe anticholinergic effects, including hallucinations, seizures, and cardiac arrhythmias.
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| Additional Infomation |
Tonilawin hydrochloride is a white crystalline powder with a slight odor. pH: 5.1-5.7 (2% aqueous solution). (NTP, 1992) Tonilawin hydrochloride belongs to the methoxybenzene class of compounds.
Thonzylamine hydrochloride is a first-generation H1 histamine receptor antagonist of the ethylenediamine class. It is an orally active antihistamine with antianaphylactic properties. It is used for the research of allergic diseases, including hypersensitivity diseases, nasal congestion, and allergic conjunctivitis. It also possesses anticholinergic properties and has been used as an antipruritic agent. |
| Molecular Formula |
C16H22N4O.CLH
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|---|---|
| Molecular Weight |
322.83300
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| Exact Mass |
322.156
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| CAS # |
63-56-9
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| Related CAS # |
91-85-0;63-56-9 (HCl);
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| PubChem CID |
6136
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2562 (rough estimate)
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| Boiling Point |
bp2.2 185-187°
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| Melting Point |
173 - 176ºC
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| Flash Point |
220.3ºC
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| Index of Refraction |
1.5800 (estimate)
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| LogP |
2.855
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
274
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CCN(CC1=CC=C(C=C1)OC)C2=NC=CC=N2.Cl
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| InChi Key |
HRYJPHOTGFERGT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H22N4O.ClH/c1-19(2)11-12-20(16-17-9-4-10-18-16)13-14-5-7-15(21-3)8-6-14;/h4-10H,11-13H2,1-3H3;1H
|
| Chemical Name |
N'-[(4-methoxyphenyl)methyl]-N,N-dimethyl-N'-pyrimidin-2-ylethane-1,2-diamine;hydrochloride
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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 | 3.0976 mL | 15.4880 mL | 30.9761 mL | |
| 5 mM | 0.6195 mL | 3.0976 mL | 6.1952 mL | |
| 10 mM | 0.3098 mL | 1.5488 mL | 3.0976 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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