Crotamiton
Based on 1 Customer Validation
Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.07%
- CAS No.: 483-63-6
- Formule: C13H17NO
- Masse moléculaire:203.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Mite |
TRPV4 |
In Vitro
Crotamiton (0-500 μM) potently inhibits GSK1016790A-activated mTRPV4 currents in HEK293T cells under the condition of 2 mM extracellular Ca2+ in vitro, with IC50 values of 15.5 μM and 16.3 μM in mouse and human, respectively[1].
Crotamiton (100-1000 μM) inhibits mTRPV4 currents activated by GSK1016790A in HEK293T cells cultured in calcium-free medium, with an IC50 of 223.5 μM[1].
Crotamiton (0-1000 μM) inhibits TRPV4 currents in GSK1016790A-activated NHEK cells in calcium-free medium[1].
Crotamiton (0-1000 μM) reduces the open probability and unitary amplitude of mTRPV4 single channels in HEK293T cells[1].
Washout after co-treatment with Crotamiton (0-1000 μM; 60 s, co-applied with GSK1016790A) and GSK1016790A induces dilation of the mTRPV4 channel in HEK293T cells, which allows the permeation of large cations up to TetMA+ (6.48 Å diameter), but does not permit the permeation of NMDG (8.90 Å diameter)[1].
Crotamiton (1 mM; 5 min pre-incubation) inhibits histamine (HY-B1204)- and chloroquine (HY-17589A)-induced calcium influx in HEK293T cells expressing H1R/TRPV1 or MRGPRA3/TRPA1, with IC50 values of 101.2 μM and 326.2 μM, respectively. Its mechanism of action functions through the H1R/TRPV1 pathway, rather than directly inhibiting TRPV1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Crotamiton (i.p., 125 mg/kg, single dose) reduces histamine- and chloroquine-induced scratching episodes in male ICR mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (male, 9-11 weeks old)[1]
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Dosage:30 μL
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Administration:topical; single dose
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Result:Significantly reduced GSK1016790A-induced scratching bouts over 15 minutes, with mean scratching bouts lower than control mice (P < 0.05).
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Animal Model:ICR mice (male, 10-11 weeks old, histamine-induced pruritus model)[2]
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Dosage:125 mg/kg
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Administration:i.p.; single dose
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Result:Reduced Histamine-induced total scratching bouts from 111.0 to 29.82.
Lowered scratching bouts measured at 10-minute intervals significantly across the 1-hour observation period.
Reduced Chloroquine-induced total scratching bouts from 286.0 to 82.20.
Lowered scratching bouts measured at 10-minute intervals significantly across the 1-hour observation period.
Chemical Information
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CAS No. 483-63-6
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Appearance <25°C Solid,>25°C Liquid
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Masse moléculaire 203.28
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Formule C13H17NO
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Color Colorless to light yellow
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SMILES
C/C=C/C(N(CC)C1=CC=CC=C1C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
In Vitro:
DMSO : 140 mg/mL (688.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 140 mg/mL (688.71 mM; Need ultrasonic)
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.5 mg/mL (17.22 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.5 mg/mL (17.22 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kittaka H, et al. Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effects. Pflugers Arch. 2017;469(10):1313-1323. [Content Brief]
[2]. Choi DS, et al. Crotamiton, an Anti-Scabies Agent, Suppresses Histamine- and Chloroquine-Induced Itch Pathways in Sensory Neurons and Alleviates Scratching in Mice. Biomol Ther (Seoul). 2020;28(6):569-575. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 4.9193 mL | 24.5966 mL | 49.1932 mL | 122.9831 mL |
| 5 mM | 0.9839 mL | 4.9193 mL | 9.8386 mL | 24.5966 mL | |
| 10 mM | 0.4919 mL | 2.4597 mL | 4.9193 mL | 12.2983 mL | |
| 15 mM | 0.3280 mL | 1.6398 mL | 3.2795 mL | 8.1989 mL | |
| 20 mM | 0.2460 mL | 1.2298 mL | 2.4597 mL | 6.1492 mL | |
| 25 mM | 0.1968 mL | 0.9839 mL | 1.9677 mL | 4.9193 mL | |
| 30 mM | 0.1640 mL | 0.8199 mL | 1.6398 mL | 4.0994 mL | |
| 40 mM | 0.1230 mL | 0.6149 mL | 1.2298 mL | 3.0746 mL | |
| 50 mM | 0.0984 mL | 0.4919 mL | 0.9839 mL | 2.4597 mL | |
| 60 mM | 0.0820 mL | 0.4099 mL | 0.8199 mL | 2.0497 mL | |
| 80 mM | 0.0615 mL | 0.3075 mL | 0.6149 mL | 1.5373 mL | |
| 100 mM | 0.0492 mL | 0.2460 mL | 0.4919 mL | 1.2298 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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