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Piroctone olamine

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Chemical Structure| 68890-66-4 同义名 : 羟吡酮 ;Piroctone ethanolamine
CAS号 : 68890-66-4
货号 : A903889
分子式 : C16H30N2O3
纯度 : 97%
分子量 : 298.421
MDL号 : MFCD01690792
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 10 mg/mL(33.51 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(167.55 mM),配合低频超声,并调节pH至9

动物实验配方:
生物活性
描述 Piroctone olamine is a pyridine derivate. It is known to have a fungicidal effect. For the C/P (climbazole/piroctone olamine) cream, the MICs were 0.625, 5, 0.625, and 2.5 mg/ml for Malassezia restricta, M. globosa, M. sympodialis, and M. slooffiae, respectively. Based on the reduced casual sebum level and extent of erythema, the antifungal activity of C/P cream against Malassezia species seems useful for the treatment of mild to moderate SD(Seborrheic dermatitis)[1]. Piroctone olamine (PO) is an ethanolamine salt of the hydroxamic acid derivative Piroctone. All Candida strains show low minimum inhibitory concentrations (MICs) for Piroctone olamine (0.125-0.5 μg/mL) and Amphotericin B (AMB) (0.03-1 μg/mL) [2]. A comparable anti-fungal effectiveness for 0.5% piroctone olamine plus 0.45% climbazole and 1% zinc pyrithione, respectively. 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[3]. Moreover, Piroctone olamine 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[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.75mL

3.35mL

1.68mL

33.51mL

6.70mL

3.35mL

参考文献

[1]Youn HJ, Kim SY, Park M, 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;28(6):733‐739

[2]do Couto FM, do Nascimento SC, Júnior SF, da Silva VK, Leal AF, Neves RP. Antifungal activity of the piroctone olamine in experimental intra-abdominal candidiasis. Springerplus. 2016;5:468. Published 2016 Apr 16

[3]Schmidt-Rose T, Braren S, Fölster H, et al. 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;33(3):276‐282

[4]Kim Y, Alpmann P, Blaum-Feder S, et al. Increased in vivo efficacy of lenalidomide by addition of piroctone olamine. In Vivo. 2011;25(1):99‐103