Piroctone-olamine-Piroctone-ethanolamine-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPiroctone olamineCat. No.: HY-B1345CAS No.: 68890-66-4Synonyms: Piroctone ethanolamine分式: CHNO分量: 298.42作靶點: Fungal作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 11.11 m

2、g/mL (37.23 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.3510 mL 16.7549 mL 33.5098 mL5 mM 0.6702 mL 3.3510 mL 6.7020 mL10 mM 0.3351 mL 1.6755 mL 3.3510 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥蔚膬湟?，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)

3、配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.11 mg/mL (3.72 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.11 mg/mL (3.72 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master o

4、f Small Molecules 您邊的抑制劑師www.MedChemESolubility: 1.11 mg/mL (3.72 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Piroctone olamine種吡啶衍物。具有殺真 作。IC50 & Target Antifungal 1體外研究 Piroctone olamine, the ethanolamine salt of the hydroxamic acid derivative Piroctone, is a hydroxypyridoneanti-mycotic agent. Piroc

5、tone olamine penetrates the cell membrane and forms complexes with iron ions,inhibiting energy metabolism in mitochondria 1. Piroctone olamine (PO) is an ethanolamine salt of thehydroxamic acid derivative Piroctone. All Candida strains show low minimum inhibitory concentrations (MICs)for Piroctone o

6、lamine (0.125-0.5 g/mL) and Amphotericin B (AMB) (0.03-1 g/mL) 2.體內(nèi)研究 This work aimed to evaluate the antifungal activity of Piroctone olamine in the treatment of intra-abdominalcandidiasis in an experimental model using Swiss mice. The treatment with Piroctone olamine (0.5 mg/kg) isperformed 72 h a

7、fter infection by intraperitoneal administration. For comparison, a group of animals (n=6) istreated with Amphotericin B (0.5 mg/kg). The mycological diagnosis is made by collecting the liver, spleenand kidneys. Data regarding the fungal growth and mortality are analyzed statistically by Students t

8、test andanalysis of variance, with level of significance set at P 2.PROTOCOLCell Assay 2 Ten different concentrations are used, ranging from 0.03 to 16 g/mL of AMB and 0.125 to 64 g/mL of FLZ.Piroctone olamine is diluted in DMSO to a stock solution concentration of 1600 g/mL. The concentrations ofPi

9、roctone olamine (PO) range from 0.0625 to 32 g/mL. The plates are incubated at 37C and readings aretaken after 24 and 48 h of incubation. Two control wells, free from other fungi and yeasts, are included in theassay. The readings are made visually for comparison against the growth in control wells.

10、The minimuminhibitory concentration (MIC) is the lowest concentration capable of inhibiting visible growth of the isolatestested against the respective control well. Assays are performed in duplicate 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Ani

11、mal Mice 2Administration 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 Piroctoneolamine (0.5 mg/kg) is performed 72 h after infection by

12、 intraperitoneal administration. For comparison, agroup of animals (n=6) is treated with Amphotericin B (0.5 mg/kg). The mycological diagnosis is made bycollecting the liver, spleen and kidneys. Data regarding the fungal growth and mortality are analyzedstatistically by Students t test and analysis

13、of variance.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. 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):733-739.2. do Couto FM, et al. Antifungal activity of the piroctone olamine in experimental intra-abdominal candidiasis. Springerplus. 2016 Apr16;5: