| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
In both cats and rabbits, chlorophenol hydrochloride (0–162 mg/kg; oral or subcutaneous injection; once) decreases respiratory fluid production [1].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Healthy, adult, male rabbit and cat [1]
Doses: 2.0, 6.0, 18, 54 and 162 mg/kg (PO) or 1.0, 3.0, 9.0, 27 and 81 mg/kg (SC) Route of Administration: Administered orally or subcutaneously (sc) (sc), once. Experimental Results: A slight but significant decrease in respiratory fluid output for one to three hrs (hrs (hours)) after administration. Fewer animals develop mucus cotton in their respiratory tracts. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Liver. Liver. |
| Toxicity/Toxicokinetics |
Toxicity Summary
It inhibits the cough reflex by acting directly on the cough center in the medulla oblongata of the brain. |
| References |
[1]. Boyd EM, et al. Chlophedianol Hydrochloride: A New Antitussive Agent. Can Med Assoc J. 1960 Dec 17;83(25):1298-301.
[2]. Paul IM. Therapeutic options for acute cough due to upper respiratory infections in children. Lung. 2012 Feb;190(1):41-4. |
| Additional Infomation |
Clofedanol is a diarylmethane compound with the structure 2-Clobenpropit(phenyl)methane, where the carbon atoms of the methane are substituted with 2-(dimethylamino)ethyl. It is used to treat dry cough by inhibiting the cough reflex through direct action on the cough center in the medulla oblongata. It is a diarylmethane and tertiary amine compound and is the conjugate base of Clofedanol (1+). Clofedanol is a centrally acting antitussive, marketed in Canada under the brand name Ulone. It is not marketed in the United States. Clofedanol is only present in individuals who have used or taken this medication. Clofedanol inhibits the cough reflex through direct action on the cough center in the medulla oblongata. Drug Indications: For the treatment of dry cough. Mechanism of Action: Inhibits the cough reflex through direct action on the cough center in the medulla oblongata.
Pharmacodynamics Clofedanol (or chlorfenapyridine) is a centrally acting antitussive. It has local anesthetic and antihistamine effects, and at high doses may have anticholinergic effects. |
| Molecular Formula |
C17H20CLNO
|
|---|---|
| Molecular Weight |
289.803
|
| Exact Mass |
289.123
|
| CAS # |
791-35-5
|
| Related CAS # |
Chlophedianol hydrochloride;511-13-7;Chlophedianol-13C6
|
| PubChem CID |
2795
|
| Appearance |
Typically exists as solid at room temperature
|
| Melting Point |
120°
|
| LogP |
3.527
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
20
|
| Complexity |
291
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Clc1c(C(CCN(C)C)(c2ccccc2)O)cccc1
|
| InChi Key |
WRCHFMBCVFFYEQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H20ClNO/c1-19(2)13-12-17(20,14-8-4-3-5-9-14)15-10-6-7-11-16(15)18/h3-11,20H,12-13H2,1-2H3
|
| Chemical Name |
1-(2-chlorophenyl)-3-(dimethylamino)-1-phenylpropan-1-ol
|
| Synonyms |
NSC113595; NSC 113595; Clofedanol
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 3.4507 mL | 17.2533 mL | 34.5066 mL | |
| 5 mM | 0.6901 mL | 3.4507 mL | 6.9013 mL | |
| 10 mM | 0.3451 mL | 1.7253 mL | 3.4507 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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