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Mefentrifluconazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mefentrifluconazole图片
CAS NO:1417782-03-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
Mefentrifluconazole 是一种新型的唑类衍生物,广谱抗真菌 (antifungal agent) 剂。Mefentrifluconazole 是具有强效选择性和口服活性真菌CYP51的抑制剂 (Kd= 0.5 nM),但是对人类芳香化酶 (IC50=0.92 μM) 的抑制活性较小。
生物活性

Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrumantifungal agent. Mefentrifluconazole is a potent, selective and orally activefungalCYP51(Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on humanaromatase(IC50=0.92 μM)[1].

IC50& Target[1]

CYP51A

0.5 nM (Kd)

体内研究
(In Vivo)

Mefentrifluconazole undergoes extensive toxicity testing, including a full program of reproductive toxicity studies. Long term repeated dose toxicity and/or carcinogenicity studies have been conducted in rats, mice, and dogs. In each species, the highest dose level investigated gives rise to systemic toxicity[1].
In the acute and repeat dose toxicity studies performed with Mefentrifluconazole. A single-dose administration to rats the LD50 is >2000 mg/kg bwt by the oral route, >5000 mg/kg bwt by the dermal route, and >5.314 mg/L by inhalation as a dust aerosol. Mefentrifluconazole is not a skin or an eye irritant, nor is it a phototoxicant in vitro[1].
In the acute neurotoxicity study in rats, Mefentrifluconazole (oral administration; 2000 mg/kg bwt; single dose) gives rise to reduce body weight gain and transient neurobehavioral effects only on the day of treatment (unsteady gait, reduced motor activity, reduces grip strength of the forelimbs and increased distance between the hind limbs in the landing foot-splay test)[1].
In the repeated-dose toxicity studies, the liver is the target organ in each of the three species investigated. At higher dose levels in the rat (oral diets; 383/334 mg/kg/bwt/d (4000 ppm)) and the C57BL/6JRj mouse (61 mg/kg bwt/d (300 ppm)), reduces body weight gain and food consumption, alters clinical chemistry parameters, increases liver weight and is accompanied by liver cell hypertrophy, and/or liver cell necrosis. At low doses, increases liver weight is not associated with any histopathological alterations and is considered to be an adaptive change to treatment[1].

分子量

397.78

性状

Solid

Formula

C18H15ClF3N3O2

CAS 号

1417782-03-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(251.40 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5140 mL12.5698 mL25.1395 mL
5 mM0.5028 mL2.5140 mL5.0279 mL
10 mM0.2514 mL1.2570 mL2.5140 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 6.25 mg/mL (15.71 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (15.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 6.25 mg/mL (15.71 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (15.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 6.25 mg/mL (15.71 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (15.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。