| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Histamine H1 receptor (antagonist); muscarinic acetylcholine receptors (anticholinergic).
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|---|---|
| ln Vitro |
In vitro, Chlorphenoxamine acts as a histamine H1 receptor antagonist, blocking the effects of histamine. It also exhibits anticholinergic activity by blocking muscarinic receptors. Quantitative in vitro activity data (e.g., IC50 or Ki values) is not detailed in publicly available sources.
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| ln Vivo |
In vivo, Chlorphenoxamine is used for the symptomatic relief of allergic conditions such as hay fever, urticaria, and pruritus. Its sedative properties are due to its ability to cross the blood-brain barrier and antagonize central H1 receptors.
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| Enzyme Assay |
No specific cell-free H1 receptor binding assay protocol is detailed for Chlorphenoxamine. For antihistamines, 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 Chlorphenoxamine and stimulated with histamine; inhibition of the response is measured.
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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). Chlorphenoxamine 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: 303.83; molecular formula: C18H22ClNO. Solubility: soluble in organic solvents; poorly soluble in water.
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| Toxicity/Toxicokinetics |
Chlorphenoxamine has been used clinically; side effects include drowsiness, dry mouth, blurred vision, and constipation due to its anticholinergic effects.
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| Additional Infomation |
Chlorphenoxamine is a diarylmethane compound with anti-coronavirus activity. It is marketed under the brand name Phenoxene. It is an antihistamine and anticholinergic drug used to treat itching and has anti-Parkinson's disease effects.
Chlorphenoxamine is an approved antihistamine in some countries, though it is not widely used today due to the availability of newer, less sedating antihistamines. It is used for allergic conditions and as an antipruritic. Its mechanism involves H1 receptor antagonism and anticholinergic effects. |
| Molecular Formula |
C18H22NOCL
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|---|---|
| Molecular Weight |
303.82638
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| Exact Mass |
303.139
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| CAS # |
77-38-3
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| Related CAS # |
562-09-4 (hydrochloride)
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| PubChem CID |
6475
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| Appearance |
Light yellow to brown liquid
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| Density |
1.093g/cm3
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| Boiling Point |
383.7ºC at 760 mmHg
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| Flash Point |
185.9ºC
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| Index of Refraction |
1.551
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| LogP |
4.181
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
296
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(CCOC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)C)C
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| InChi Key |
KKHPNPMTPORSQE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22ClNO/c1-18(21-14-13-20(2)3,15-7-5-4-6-8-15)16-9-11-17(19)12-10-16/h4-12H,13-14H2,1-3H3
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| Chemical Name |
2-[1-(4-chlorophenyl)-1-phenylethoxy]-N,N-dimethylethanamine
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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) |
DMSO : ≥ 48 mg/mL (~157.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2913 mL | 16.4566 mL | 32.9131 mL | |
| 5 mM | 0.6583 mL | 3.2913 mL | 6.5826 mL | |
| 10 mM | 0.3291 mL | 1.6457 mL | 3.2913 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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