Crotamiton
(Synonyms: 克罗米通) 目录号 : GC32274
An ectoparasiticide and antipruritic
Cas No.:483-63-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Crotamiton is an ectoparasiticide and antipruritic agent.1,2,3 It blocks the mouse transient receptor potential vanilloid 4 (TRPV4) channel expressed in HEK293 cells in a calcium-dependent manner (IC50s = 223.5 and 15.5 μM in buffer containing 0 and 2 mM calcium, respectively).2 It inhibits scratching behavior in mice induced by the TRPV4 agonist GSK1016790A . Topical application of crotamiton (0.025 g of a 10% ointment) also inhibits scratching behavior in mice induced by histamine, serotonin , and the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 .3 Formulations containing crotamiton have been used to eradicate scabies and in the treatment of symptomatic pruritic skin.
1.Goldust, M., Rezaee, E., and Raghiafar, R.Topical ivermectin versus crotamiton cream 10% for the treatment of scabiesInt. J. Dermatol.53(7)904-908(2014) 2.Kittaka, H., Yamanoi, Y., and Tominaga, M.Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effectsPflugers Arch.469(10)1313-1323(2017) 3.Sekine, R., Satoh, T., Takaoka, A., et al.Anti pruritic effects of topical crotamiton, capsaicin, and a corticosteroid on pruritogen-induced scratching behaviorExp. Dermatol.21(3)201-204(2012)
| Cas No. | 483-63-6 | SDF | |
| 别名 | 克罗米通 | ||
| Canonical SMILES | C/C=C/C(N(CC)C1=CC=CC=C1C)=O | ||
| 分子式 | C13H17NO | 分子量 | 203.28 |
| 溶解度 | DMSO : ≥ 58 mg/mL (285.32 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Scabies: Epidemiology, Diagnosis, and Treatment
Dtsch Arztebl Int 2021 Oct 15;118(41):695-704.PMID:34615594DOI:10.3238/arztebl.m2021.0296.
Background: Scabies is a skin infestation whose incidence is apparently rising. Methods: This review is based on pertinent articles retrieved by a selective search of PubMed on diagnosis and treatment strategies. Results: Thread-like papules (burrows), new, intense pruritus, and dermatitis guide the suspected diagnosis which is confirmed by the microscopic or dermatoscopic demonstration of scabies mites. The first line therapy is topical application of permethrin, in accordance with the current recommendations for its use. Other treatment options include systemic ivermectin and topical Crotamiton or benzyl benzoate. A combination of permethrin and ivermectin is used to treat otherwise intractable cases and is generally indicated for the treatment of crusted scabies. Known causes of treatment failure include improper application of the external agents, failure of repeated treatment with ivermectin, incomplete decontamination of furnishings and clothes, failure to simultaneously treat contact persons, absence of written documents explaining treatment modalities, and the patient's belonging to a risk group. Even though there has not yet been any direct proof of resistance of scabies mites to permethrin, there is a rising number of welldocumented cases of poor response to this agent. Moxidectin is a new substance now undergoing clinical testing. Conclusion: Treatment of scabies according to the guidelines and the additional recommendations reported here should result in effective curing, even in cases that are thought to be intractable.
Crotamiton derivative JM03 extends lifespan and improves oxidative and hypertonic stress resistance in Caenorhabditis elegans via inhibiting OSM-9
Elife 2022 May 5;11:e72410.PMID:35510610DOI:10.7554/eLife.72410.
While screening our in-house 1072 marketed drugs for their ability to extend the lifespan using Caenorhabditis elegans (C. elegans) as an animal model, Crotamiton (N-ethyl-o-crotonotoluidide) showed anti-aging activity and was selected for further structural optimization. After replacing the ortho-methyl of Crotamiton with ortho-fluoro, Crotamiton derivative JM03 was obtained and showed better activity in terms of lifespan-extension and stress resistance than Crotamiton. It was further explored that JM03 extended the lifespan of C. elegans through osmotic avoidance abnormal-9 (OSM-9). Besides, JM03 improves the ability of nematode to resist oxidative stress and hypertonic stress through OSM-9, but not osm-9/capsaicin receptor related-2 (OCR-2). Then the inhibition of OSM-9 by JM03 reduces the aggregation of Q35 in C. elegans via upregulating the genes associated with proteostasis. SKN-1 signaling was also found to be activated after JM03 treatment, which might contribute to proteostasis, stress resistance and lifespan extension. In summary, this study explored a new small molecule derived from Crotamiton, which has efficient anti-oxidative, anti-hypertonic, and anti-aging effects, and could further lead to promising application prospects.
Crotamiton, an Anti-Scabies Agent, Suppresses Histamine- and Chloroquine-Induced Itch Pathways in Sensory Neurons and Alleviates Scratching in Mice
Biomol Ther (Seoul) 2020 Nov 1;28(6):569-575.PMID:32536619DOI:10.4062/biomolther.2020.063.
Crotamiton is an anti-scabies drug, but it was recently found that Crotamiton also suppresses non-scabietic itching in mice. However, the underlying mechanism is largely unclear. Therefore, aim of the study is to investigate mechanisms of the anti-pruritic effect of Crotamiton for non-scabietic itching. Histamine and chloroquine are used as non-scabietic pruritogens. The effect of Crotamiton was identified using fluorometric intracellular calcium assays in HEK293T cells and primary cultured dorsal root ganglion (DRG) neurons. Further in vivo effect was evaluated by scratching behavior tests. Crotamiton strongly inhibited histamine-induced calcium influx in HEK293T cells, expressing both histamine receptor 1 (H1R) and transient receptor potential vanilloid 1 (TRPV1), as a model of histamine-induced itching. Similarly, it also blocked chloroquine-induced calcium influx in HEK293T cells, expressing both Mas-related G-protein-coupled receptor A3 (MRGPRA3) and transient receptor potential A1 (TRPA1), as a model of histamine-independent itching. Furthermore, Crotamiton also suppressed both histamine- and chloroquine-induced calcium influx in primary cultures of mouse DRG. Additionally, Crotamiton strongly suppressed histamine- and chloroquine-induced scratching in mice. Overall, it was found that Crotamiton has an anti-pruritic effect against non-scabietic itching by histamine and chloroquine. Therefore, Crotamiton may be used as a general anti-pruritic agent, irrespective of the presence of scabies.
Removal of Crotamiton and its degradation intermediates from secondary effluent using TiO2-zeolite composites
Water Sci Technol 2018 Feb;77(3-4):788-799.PMID:29431724DOI:10.2166/wst.2017.578.
Crotamiton, a scabicide and antipruritic agent persistent during biological treatment processes, is frequently detected in secondary effluent. In this study, titanium dioxide (TiO2) and high-silica zeolite (HSZ-385) composites were synthesized and applied for the treatment of Crotamiton in secondary effluent. Crotamiton was rapidly adsorbed by HSZ-385, and the adsorption performance of Crotamiton in the secondary effluent was quite close to that in the test using ultrapure water. Even though the TiO2-zeolite composites showed lower adsorption rates than that of HSZ-385, similar Crotamiton adsorption capacities were revealed using both test materials. The photocatalytic decomposition of Crotamiton was significantly inhibited by the water matrix at low initial concentrations. The TiO2-zeolite composites rapidly adsorbed Crotamiton from secondary effluent, and then the Crotamiton was gradually decomposed under ultraviolet irradiation. Importantly, when using TiO2-zeolite composites, coexisting material in the secondary effluent did not markedly inhibit Crotamiton removal at low initial Crotamiton concentration. The behaviors of the main intermediates during treatment demonstrated that the main degradation intermediates of Crotamiton were also captured by the composites.
The Treatment of Scabies
Dtsch Arztebl Int 2016 Nov 14;113(45):757-762.PMID:27974144DOI:10.3238/arztebl.2016.0757.
Background: Scabies is a contagious infestation transmitted by skin-to-skin contact and sometimes by contact with contaminated material. The scabies mite burrows into the skin, producing a papular rash and severe itch at typical sites of predilection. Methods: We systematically reviewed the literature to compare the efficacy of various anti-scabies agents, including a calculation of relative risks and confidence intervals. Results: A literature search yielded 596 initial hits; after screening in accor-dance with the defined inclusion and exclusion criteria, 16 studies were selected for this review. Among topical treatments for scabies, permethrin was equally effective or more effective than Crotamiton or benzyl benzoate. In a comparison of topical versus systemic treatment, topical permethrin and systemic ivermectin did not differ substantially in efficacy (7 comparative studies revealed no difference; one revealed a difference in favor of permethrin). Comparative trials of topical benzyl benzoate versus systemic ivermectin yielded inconsistent findings. Single and double administrations of ivermectin were similarly effective. In trials involving entire populations with a high prevalence of scabies, systemic ivermectin was found to be superior to topical permethrin. Conclusion: There are hardly any differences in efficacy between the available treatments for scabies. Single administrations of permethrin 5%, Crotamiton 10%, and systemic ivermectin are all comparably effective. There are differences in the frequeny and ease of application as well as when eradicating scabies in populations with a high prevalence.