| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Crotamiton targets TRPV4 (transient receptor potential vanilloid 4) channels. It acts as a TRPV4 inhibitor, blocking TRPV4-mediated currents. It also functions as both an activator and inhibitor of Cytochrome P450 3A4 with a potency of 12589.3 nM. It may also interact with H1R/TRPV1 pathways.
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|---|---|
| ln Vitro |
Crotamiton inhibits TRPV4 currents. It inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. It inhibits histamine- and chloroquine-induced pruritus. It has antibacterial properties.
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| ln Vivo |
Crotamiton is used as a scabicidal agent for the eradication of scabies (Sarcoptes scabiei). It is also used for the symptomatic treatment of pruritic skin. It relieves itching by producing a counter-irritation effect.
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| Enzyme Assay |
Crotamiton is evaluated in cell-free assays for its ability to inhibit TRPV4 channel activity. The compound is incubated with TRPV4-expressing membranes or purified TRPV4 protein, and channel activity is measured using electrophysiological or flux assays. IC50 values are determined to quantify the potency of TRPV4 inhibition.
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| Cell Assay |
Crotamiton is assessed in cell-based assays using cells expressing TRPV4 channels. Cells are treated with Crotamiton, and TRPV4-mediated calcium influx is measured using fluorescence-based calcium imaging. The compound's ability to inhibit TRPV4 agonist-induced responses is evaluated.
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| Animal Protocol |
Crotamiton is administered topically in animal models to evaluate its antipruritic and scabicidal effects. It inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Efficacy is assessed by measuring scratching behavior and skin lesion improvement.
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| ADME/Pharmacokinetics |
Crotamiton has a molecular weight of 203.28 and a molecular formula of C13H17NO. It has a CAS number of 483-63-6. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Crotamiton beyond its known use as a topical agent. The compound is for research use only and is not intended for human therapeutic use. It is a topical medication and is generally well-tolerated.
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| Additional Infomation |
Crotamiton is an enamide formed by the condensation of crotonic acid and N-ethyl-2-methylaniline. It is a colorless or pale yellow oily liquid used to treat itching. Its mechanism of action is through counter-stimulation: when it evaporates from the skin, it produces a cooling sensation, thus diverting attention from the itching. It has also been used as a mite-killing agent for scabies, but more effective medications are generally preferred. It is both an antipruritic and an anti-scabies agent. It is an enamide and also a tertiary amide.
See also: Crotamiton (note moved to). Crotamiton is used as a scabicide and antipruritic agent. It is also known as Crotan and Eurax. It is a TRPV4 inhibitor. It is not approved for clinical use in all regions. |
| Molecular Formula |
C13H17NO
|
|---|---|
| Molecular Weight |
203.28
|
| Exact Mass |
203.131
|
| CAS # |
483-63-6
|
| PubChem CID |
688020
|
| Appearance |
Colorless to light yellow <25°C solid powder,>25°C liquid
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
282.7±19.0 °C at 760 mmHg
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| Flash Point |
115.5±12.7 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.552
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
15
|
| Complexity |
235
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C/C=C/C(N(CC)C1=CC=CC=C1C)=O
|
| InChi Key |
DNTGGZPQPQTDQF-XBXARRHUSA-N
|
| InChi Code |
InChI=1S/C13H17NO/c1-4-8-13(15)14(5-2)12-10-7-6-9-11(12)3/h4,6-10H,5H2,1-3H3/b8-4+
|
| Chemical Name |
(E)-N-ethyl-N-(2-methylphenyl)but-2-enamide
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| Synonyms |
Crotamitone; N-Ethyl-o-crotonotoluidide; Crotamiton
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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)
|
| Solubility (In Vitro) |
DMSO : ~140 mg/mL (~688.71 mM)
H2O : ~140 mg/mL (~688.71 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.5 mg/mL (17.22 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 35.0 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: ≥ 3.5 mg/mL (17.22 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 35.0 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: ≥ 3.5 mg/mL (17.22 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 | 4.9193 mL | 24.5966 mL | 49.1932 mL | |
| 5 mM | 0.9839 mL | 4.9193 mL | 9.8386 mL | |
| 10 mM | 0.4919 mL | 2.4597 mL | 4.9193 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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