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Olorofim

产品编号 T27300 CAS 1928707-56-5

别名: Olorofim, F901318, F-901318

Olorofim 是一种新型的选择性抗真菌化合物，对烟曲霉DHODH 具有抑制作用（IC50：44 nM），对人类DHODH 几乎没有抑制作用（<100 uM）。Olorofim 对青霉菌属、皮炎杆菌属、镰刀菌属等各种致病性丝状和二形真菌有很好的疗效。

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Olorofim, CAS 1928707-56-5

规格	价格/CNY	货期
1 mg	￥ 2,720	现货
5 mg	￥ 6,390	现货
10 mg	￥ 8,680	现货
25 mg	￥ 12,500	现货
50 mg	￥ 15,900	现货
100 mg	￥ 19,600	现货
500 mg	￥ 39,200	现货

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选择批次

纯度: 99.28%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Olorofim is a novel selective antifungal compound with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM) and almost no inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against various pathogenic filamentous and dimorphic fungi such as Penicillium spp, Dermatophilus spp and Fusarium spp.
靶点活性	Talaromyces species/Trichophyton species:0.015 mg/L(MIC), Penicillium:0.027 mg/L(MIC), Cryptic aspergillis:0.004-0.03 mg/L(MIC), Trichophyton isolates:0.008 mg/L(MIC), Dermatophytes and opportunistic moulds:0.004-0.125 mg/L(MIC)
体外活性	Olorofim (0.004-0.125 mg/L) showed highly potent in vitro activity against dermatophytes and opportunistic moulds (MIC range of 0.004-0.125 mg/L) except for Alternaria alternata. Penicillium, and Talaromyces species and Trichophyton species exhibited a low geometric mean (GM) MIC (GM 0.027 mg/L and 0.015 mg/L, respectively) of olorofim. Importantly, a 2-12 dilution step decrease in in vitro activity of olorofim as compared with azoles was observed against Penicillium and Talaromyces. Notably, olorofim displayed potent in vitro activity against Trichophyton isolates including terbinafine-resistant and azole-resistant Trichophyton mentagrophytes/interdigitale with a modal MIC value of 0.008 mg/L. Further, azole-resistant A. fumigatus isolates harbouring mutations in azole target Cyp51A genes and several cryptic aspergilli displayed low MICs (range 0.004-0.03 mg/L) of olorofim.[2]
体内活性	The in vivo efficacy of the drug was investigated, using a guinea pig model, experimentally infected with Microsporum gypseum. Typical skin lesions of dermatophyte infection were observed in the guinea pig model at 7 days postinoculation. Following 1 week of daily topical administration of olorofim, similar to the clotrimazole group, the skin lesions were resolved and normal hair growth patterns appeared.[1]

别名	Olorofim, F901318, F-901318
分子量	498.55
分子式	C28H27FN6O2
CAS No.	1928707-56-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (100.29 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0058 mL	10.0291 mL	20.0582 mL	50.1454 mL
	5 mM	0.4012 mL	2.0058 mL	4.0116 mL	10.0291 mL
	10 mM	0.2006 mL	1.0029 mL	2.0058 mL	5.0145 mL
	20 mM	0.1003 mL	0.5015 mL	1.0029 mL	2.5073 mL
	50 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0029 mL
	100 mM	0.0201 mL	0.1003 mL	0.2006 mL	0.5015 mL

计算器

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分子量计算器

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参考文献

1. Mirbzadeh Ardakani E, et al. Olorofim Effectively Eradicates Dermatophytes In Vitro and In Vivo. Antimicrob Agents Chemother. 2021;65(12):e0138621. 2. Oliver JD, Sibley GE, Beckmann N, Dobb KS, Slater MJ, McEntee L, du Pré S, Livermore J, Bromley MJ, Wiederhold NP, Hope WW, Kennedy AJ, Law D, Birch M. F901318 represents a novel class of antifungal drug that inhibits dihydroorotate dehydrogenase. Proc Natl Acad Sci U S A. 2016 Oct 25. pii: 201608304. [Epub ahead of print] PubMed PMID: 27791100; PubMed Central PMCID: PMC5111691. 3. Singh A, et al. In vitro activity of the novel antifungal olorofim against dermatophytes and opportunistic moulds including Penicillium and Talaromyces species. J Antimicrob Chemother. 2021;76(5):1229-1233. 4. Lim W, et al. Madurella mycetomatis, the main causative agent of eumycetoma, is highly susceptible to olorofim. J Antimicrob Chemother. 2020;75(4):936-941.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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