Piroctone olamine (Piroctone ethanolamine)
(Synonyms: 吡罗克酮乙醇胺盐; Piroctone ethanolamine) 目录号 : GC32203
Piroctone Olamine (piroctone ethanolamine) is a wide spectrum antibacterial and antifungal agent used in the treatment of dandruff,fungal infections.
Cas No.:68890-66-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
Ten different concentrations are used, ranging from 0.03 to 16 μg/mL of AMB and 0.125 to 64 μg/mL of FLZ. Piroctone olamine is diluted in DMSO to a stock solution concentration of 1600 μg/mL. The concentrations of Piroctone olamine (PO) range from 0.0625 to 32 μg/mL. The plates are incubated at 37°C and readings are taken after 24 and 48 h of incubation. Two control wells, free from other fungi and yeasts, are included in the assay. The readings are made visually for comparison against the growth in control wells. The minimum inhibitory concentration (MIC) is the lowest concentration capable of inhibiting visible growth of the isolates tested against the respective control well. Assays are performed in duplicate[2]. |
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Animal experiment: |
Mice[2] The swiss mice (n=6) are infected by intraperitoneal injection of 0.2 mL of C. albicans (107cells/ml in saline). The animals are observed daily for clinical signs and mortality for 14 days. The treatment with Piroctone olamine (0.5 mg/kg) is performed 72 h after infection by intraperitoneal administration. For comparison, a group of animals (n=6) is treated with Amphotericin B (0.5 mg/kg). The mycological diagnosis is made by collecting the liver, spleen and kidneys. Data regarding the fungal growth and mortality are analyzed statistically by Student’s t test and analysis of variance. |
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References: [1]. Youn HJ, et al. Efficacy and Safety of Cream Containing Climbazole/Piroctone Olamine for Facial Seborrheic Dermatitis: A Single-Center, Open-Label Split-Face Clinical Study. Ann Dermatol. 2016 Dec;28(6):733-739. |
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Piroctone Olamine (piroctone ethanolamine) is a wide spectrum antibacterial and antifungal agent used in the treatment of dandruff,fungal infections.
| Cas No. | 68890-66-4 | SDF | |
| 别名 | 吡罗克酮乙醇胺盐; Piroctone ethanolamine | ||
| Canonical SMILES | O=C1C=C(C)C=C(CC(C)CC(C)(C)C)N1O.NCCO | ||
| 分子式 | C16H30N2O3 | 分子量 | 298.42 |
| 溶解度 | DMSO : 11.11 mg/mL (37.23 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 | 3.351 mL | 16.7549 mL | 33.5098 mL |
| 5 mM | 0.6702 mL | 3.351 mL | 6.702 mL |
| 10 mM | 0.3351 mL | 1.6755 mL | 3.351 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。
Fe3O4@Piroctone olamine magnetic nanoparticles: Synthesize and therapeutic potential in cutaneous leishmaniasis
Biomed Pharmacother 2021 Jul;139:111566.PMID:33839494DOI:10.1016/j.biopha.2021.111566.
Background: In recent years, magnetic nanoparticles (NMP) as novel materials have been widely used for biomedical, diagnostic and therapeutic purposes like microbial infection therapy. The purpose of this study is to synthesize PO coated iron oxide magnetic nanoparticles (Fe3O4@PO NPs) and their anti-leishmanial effects in vitro and in vivo against cutaneous leishmaniasis. Methods: Fe3O4 magnetic nanoparticles were synthesized by the coprecipitation of Fe2 + and Fe3 + ions and used as a nanocarrier for the production of Fe3O4@PO NPs. The in vitro antileishmanial effects of PO-coated Fe3O4 NPs and Fe3O4 NPs (10-200 碌g/mL) was determined against the intracellular amastigotes of Leishmania major (MRHO/IR/75/ER) and, then, examined on cutaneous leishmaniasis induced in male BALB/c mice by L. major. The rate of infectivity, production of nitric oxide (NO), and cytotoxic activates of Fe3O4 NPs and Fe3O4@PO NPs on J774-A1 macrophage cells were determined. Results: The size scattering of the Fe3O4 NPs and Fe3O4@PO NPs were in the range among 1-40 and 5-55 nm, respectively. The obtained IC50 values were 62.3 卤 2.15 渭g/mL, 31.3 卤 2.26 渭g/mL, and 52.6 卤 2.15 渭g/mL for the Fe3O4 NPs and Fe3O4@PO NPs, and MA, respectively. The results revealed that the mean number of parasites and the mean diameter of the lesions was considerably (p < 0.05) decreased in the infected mice treated with Fe3O4 NPs and Fe3O4@PO NPs. The Fe3O4 NPs and Fe3O4@PO NPs significantly (p < 0.05) prompted the production of NO as a dose-dependent manner. The promastigotes pre-incubated in Fe3O4 NPs and Fe3O4@PO NPs at the concentration of 5 碌g/mL had the ability to infect only 41.7% and 28.3% of the macrophages cells. The selectivity index of greater than 10 for Fe3O4 NPs and Fe3O4@PO NPs showed its safety to the J774-A1 macrophage cells and specificity to the parasite. Conclusion: The results of this survey indicated the high potency of Fe3O4@PO NPs to inhibit the growth of amastigote forms of L. major as well as recovery and improvement CL induced by L. major in BALB/c mice without significant cytotoxicity. The results also indicated that, although the possible anti-leishmanial mechanisms of Fe3O4@PO NPs have not been clearly understood, however, the triggering of NO may be considered as one of the possible anti-leishmanial mechanisms of these nanoparticles. However, additional studies, in particular in clinical contexts, are mandatory.
The effect of Piroctone olamine on reproduction of male and female rats
Fundam Appl Toxicol 1991 Jan;16(1):31-40.PMID:2019350DOI:10.1016/0272-0590(91)90132-n.
The purpose of this study was to determine the effect of Piroctone olamine, an antidandruff active, on reproductive performance, fertility, parturition, and neonatal viability and growth. Piroctone olamine was administered orally by gavage to three groups of 35 male Sprague-Dawley rats each beginning 64 days prior to mating and continuing until euthanized and to three groups of 35 female Sprague-Dawley rats each beginning 14 days prior to mating and continuing until euthanized. Animals in the treated groups received Piroctone olamine in a combination of 1.0% methylcellulose and polyethylene glycol 400 as a single daily dose at levels of 0, 10, 100, and 250 mg/kg/day, at a volume of 2.5 ml/kg. The control group received the vehicle only. Ten randomly selected females/group were mated and underwent a uterine examination on Gestation Day 13; the remaining females were allowed to deliver. Because earlier studies reported hematological effects, blood samples were collected from all parental animals during acclimation and prior to euthanasia for hematological and blood chemistry (Gestation Day 13 females) characterization. The parental animals were necropsied and tissues were grossly examined. Systemic effects induced by the test article were seen at the mid- and high-dose levels but only among the male rats. These effects were reduced body weight and decreased liver weights. Hematological findings representative of anemia occurred at the high-dose level, as did rales in several animals. Offspring growth was inhibited for the high-dose group as evidenced by significantly reduced mean weight values throughout lactation. The remaining parameters assessed, including mating ability and reproductive performance, were not affected by treatment at any dosage level tested. In summary, the no observable effect level of Piroctone olamine with respect to systemic toxicity was considered to be 10 mg/kg/day. Neonatal growth was not affected at 100 mg/kg/day or less, and the no observable effect level with respect to reproductive parameters, including fertility, was 250 mg/kg/day.
Efficacy of a Piroctone olamine/climbazol shampoo in comparison with a zinc pyrithione shampoo in subjects with moderate to severe dandruff
Int J Cosmet Sci 2011 Jun;33(3):276-82.PMID:21272039DOI:10.1111/j.1468-2494.2010.00623.x.
Dandruff is a chronic scalp disorder characterized by scaling and itching. A successful anti-dandruff shampoo not only has to provide superior anti-dandruff relief to ensure patient compliance. It also needs to offer excellent cosmetic and hair conditioning benefits at the same time. In this study, the efficacy of a shampoo containing 0.5% Piroctone olamine and 0.45% climbazole (shampoo 1) was compared with a widely available commercial shampoo containing 1% zinc pyrithione (shampoo 2). In vitro studies investigating the anti-mycotic efficacy of a combination of 0.5% Piroctone olamine and 0.45% climbazole as well as 1% zinc pyrithione were performed. To study substantivity, pig skin punches were used as a model system and a test of wet combability was performed to characterize combing ease. In vivo home-in-use studies were carried out to determine the efficacy of both shampoos to improve scalp condition and reduce itching in subjects suffering from moderate to severe dandruff. Results demonstrated a comparable anti-fungal effectiveness for 0.5% Piroctone olamine plus 0.45% climbazole and 1% zinc pyrithione, respectively. Shampoo 1 showed a significantly higher anti-mycotics substantivity compared to shampoo 2. After treatment with shampoo 1, the wet combing force was significantly reduced compared with shampoo 2, suggesting a better combability following the use of shampoo 1. In an in vivo split head design study, shampoo 1 was shown to be equally effective in reducing the amount of dandruff on the scalp compared with shampoo 2. The approval rate of volunteers regarding the question 'The use of this shampoo decreases the itching of my scalp?' after a 4-week treatment with shampoo 1 equaled 90%. Overall, the shampoo formulation with 0.5% Piroctone olamine and 0.45% climbazole effectively reduces the amount of dandruff and, at the same time, provides hair conditioning advantages.
Increased in vivo efficacy of lenalidomide by addition of Piroctone olamine
In Vivo 2011 Jan-Feb;25(1):99-103.PMID:21282741doi
Background: It was recently confirmed that the antifungal agent ciclopirox olamine inhibits Wnt/beta catenin signaling in myeloma. Piroctone olamine (PO) has very similar chemical features to ciclopirox olamine. Materials and methods: This study investigated the antitumor effect of PO in vitro and in vivo in a murine myeloma model. Results: PO demonstrated a major apoptotic activity in various human and murine myeloma and lymphoma cell lines, as well as in human primary cells. In vivo, tumor growth, as well as overall survival, was significantly reduced in mice treated with PO as compared to untreated mice. Interestingly, concerning tumor growth and survival of the animals, a significant additive effect was seen by the combination of lenalidomide plus PO as compared to single application. Conclusion: These results reveal a significant selective induction of apoptosis by PO and suggest a significant in vivo effect against myeloma.
Scalp application of the antioxidant Piroctone olamine reduces hair shedding in an 8-week randomized, double-blind, placebo-controlled clinical study
Int J Cosmet Sci 2021 Nov;43 Suppl 1:S26-S33.PMID:34424549DOI:10.1111/ics.12737.
Objective: Increasing scalp hair fullness is a global unmet consumer need. An approach to decrease hair shedding by reducing scalp stratum corneum oxidation via a combination of antioxidant and barrier-enhancing technologies has been previously demonstrated. The purpose of this study was to test the effectiveness of the individual antioxidant Piroctone olamine in two different product forms (shampoo or leave-on product) for activity to improve hair retention. Methods: Female subjects with self-perceived hair thinning participated in an 8-week, double-blind, placebo-controlled, randomized clinical study to evaluate either a Piroctone olamine (PO) containing shampoo or a PO containing leave on treatment, each relative to their corresponding placebo formulation Too many periods. Results for phototrichograms, TEWL, and biomarker analysis of scalp condition for the shampoo treatments are discussed. Phototrichogram results are shared for the assessment of the leave on treatment. Results: Statistically significant increases in hair amount were observed by phototrichogram after use of both PO-containing products versus placebo formulations. The PO shampoo treatment also significantly decreased oxidative stress on the hair and scalp, and improved scalp condition as assessed by TEWL and scalp biomarker values. Conclusion: These results illustrate the effectiveness of a cosmetic antioxidant to improve scalp condition thereby improving hair retention. The observed improvements in scalp condition are consistent with previous reports with other antioxidant technologies and suggest that the hair retention effect was achieved by preventing oxidative damage to the scalp.