| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| Targets |
Chlorcyclizine primarily functions as a competitive antagonist of the histamine H1 receptor. By binding to these receptors, it prevents histamine from exerting its physiological effects such as vasodilation, smooth muscle contraction, and increased vascular permeability. Additionally, Chlorcyclizine has been identified as an HCV entry inhibitor, targeting viral entry mechanisms. It also exhibits anticholinergic activity via muscarinic receptor antagonism.
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| ln Vitro |
In vitro, Chlorcyclizine demonstrates potent H1 receptor antagonism with a Ki of 9 nM. It inhibits HCV entry with an EC50 of 44 nM and shows synergistic antiviral effects when combined with direct-acting antivirals (DAAs). The compound exhibits preferential liver accumulation (liver-to-plasma ratio >10). It also demonstrates antimicrobial activity and can be used as an antiseptic, particularly for the treatment of eye infections.
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| ln Vivo |
Rats in pregnancy that were given chlorcyclizine at doses of 30, 60, and 90 mg/kg at the delicate stage of palate development lived until their planned sacrifice on gestation day (GD) 17 or 21. Rats given 60 or 90 mg/kg of chlorcyclizine experienced 7% and 7% body weight loss, respectively, between doses, as well as temporary unfavorable clinical symptoms (rhinorrhea, red perioral material, urogenital staining, and loose stools). 11%. Rats given 30 mg/kg of chlorcyclizine during gestation did not acquire weight at the anticipated dose intervals, but they did not exhibit any negative clinical symptoms. Testing facility-based historical control database (16 studies, n = 380). Rats that are pregnant usually gain between 12 and 15 weeks of body weight [1].
In vivo, Chlorcyclizine demonstrates a long duration of action and mild sedative properties. It is effective as an antihistamine for the relief of allergic symptoms such as sneezing, itching, and runny nose. The compound has been studied for its antiviral activity in animal models of HCV infection, showing potential for drug repurposing. Its preferential liver accumulation supports its use as an antiviral agent targeting hepatic infections. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for H1 receptor antagonism typically use radioligand binding assays with [³H]mepyramine as the labeled ligand. Membranes prepared from mammalian brain or cells expressing human H1 receptors are incubated with the radioligand and varying concentrations of Chlorcyclizine. Specific binding is determined by subtracting non-specific binding (defined by excess unlabeled mepyramine or triprolidine). Ki values are calculated from competition binding curves using the Cheng-Prusoff equation.
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| Cell Assay |
Cellular assays for antiviral activity typically use HCV cell culture systems such as Huh7.5 cells infected with HCV genotype 2a (JFH-1) or other genotypes. Cells are treated with Chlorcyclizine at various concentrations, and viral replication is measured by quantifying HCV RNA or viral proteins (e.g., NS5A or core protein) using qRT-PCR or immunoassay. EC50 values for inhibition of HCV entry or replication are calculated from dose-response curves. Combinations with DAAs are tested for synergistic effects.
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| Animal Protocol |
In vivo animal studies for antihistamine activity typically use rodent models of allergic reactions such as histamine-induced cutaneous wheal or anaphylaxis. Animals are administered Chlorcyclizine orally or intraperitoneally at various doses prior to histamine challenge. The reduction in wheal size or anaphylactic response is measured. For antiviral studies, HCV mouse models (e.g., transgenic or humanized liver mice) are used to assess in vivo efficacy. Viral load and liver enzyme levels are monitored.
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| ADME/Pharmacokinetics |
Chlorcyclizine exhibits a distinct pharmacokinetic profile compared to related compounds such as cyclizine and meclizine. It demonstrates preferential liver accumulation with a liver-to-plasma ratio greater than 10. The compound is orally bioavailable and has a long duration of action, supporting once- or twice-daily dosing. It is metabolized in the liver and excreted primarily via the kidneys. Detailed PK parameters are available from published pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
Chlorcyclizine is generally well-tolerated at therapeutic doses, with mild sedative properties being the most common side effect. Anticholinergic effects such as dry mouth, blurred vision, and urinary retention may occur, particularly at higher doses. The compound has a long history of clinical use as an antihistamine, and its safety profile is well-established. In antiviral applications, preclinical toxicity studies would be required to assess safety margins for the new indication.
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| References | |
| Additional Infomation |
Depending on state or federal labeling requirements, Chlorcyclizine hydrochloride may cause developmental toxicity. It is a histamine H1 receptor antagonist with weak sedative effects but often causes gastrointestinal irritation. It is used to treat asthma, hay fever, urticaria, and rhinitis, and is also used in veterinary medicine. Triperamine can be administered via various routes, including topical application. See also: Chlorcyclizine (containing the active ingredient)...see more...
Chlorcyclizine is a first-generation antihistamine with a long history of clinical use for allergic conditions. It has been repurposed as an HCV entry inhibitor, demonstrating potent antiviral activity with an EC50 of 44 nM and synergistic effects with DAAs. The compound exhibits preferential liver accumulation, making it attractive for hepatic antiviral applications. It also has anticholinergic, antiemetic, and local anesthetic activities. Chlorcyclizine is available for research use and has been studied in drug repurposing contexts. |
| Molecular Formula |
C18H21N2CL.HCL
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|---|---|
| Molecular Weight |
337.28668
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| Exact Mass |
336.115
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| CAS # |
14362-31-3
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| Related CAS # |
Chlorcyclizine;82-93-9
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| PubChem CID |
62413
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| Appearance |
White to off-white solid powder
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| Density |
1.145g/cm3
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| Boiling Point |
393.6ºC at 760mmHg
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| Flash Point |
191.9ºC
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| Vapour Pressure |
2.1E-06mmHg at 25°C
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| Index of Refraction |
1.59
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| LogP |
4.354
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
300
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl
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| InChi Key |
MSIJLVMSKDXAQN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21ClN2.ClH/c1-20-11-13-21(14-12-20)18(15-5-3-2-4-6-15)16-7-9-17(19)10-8-16;/h2-10,18H,11-14H2,1H3;1H
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| Chemical Name |
1-[(4-chlorophenyl)-phenylmethyl]-4-methylpiperazine;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) |
DMSO : ~77.5 mg/mL (~229.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (7.65 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 25.8 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: ≥ 2.58 mg/mL (7.65 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 25.8 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: ≥ 2.58 mg/mL (7.65 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 | 2.9648 mL | 14.8240 mL | 29.6481 mL | |
| 5 mM | 0.5930 mL | 2.9648 mL | 5.9296 mL | |
| 10 mM | 0.2965 mL | 1.4824 mL | 2.9648 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02118012
Conditions:Chronic Hepatitis CProducts are for research use only; We do not sell to patients
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