烯酰吗啉对辣椒疫霉、柑橘疫霉和寄生疫霉菌的 EC50 分别低于 0.1 µg/mL、0.14 µg/mL 和 0.38 µg/mL，抑制这些卵菌 [1]。尽管烯酰吗啉在酵母抗雄激素筛选中不会降低 AR 活性（IC50 = 0.263 和 38.5 µM），但在 MDA-kb2 人乳腺癌细胞的报告测定中却会降低 AR 活性 [2]。

Absorption, Distribution and Excretion
Rat Oral administration of dimethomorph (10 mg/kg single dose; 10 mg/kg 14-day repeated dose; 10 mg/kg 7-day repeated dose; 500 mg/kg single dose) results in rapid excretion into the urine and feces of rats. For all treatment protocols, most (80-90%) of the radiolabel administered was excreted in the feces. A considerably smaller amount (6-16%) was excreted in the urine and only minimal levels (0.1-0.4%) were detected in the organs and tissues. Rapid absorption may be inferred by the rapid excretion of metabolites in the urine and bile. Saturation of absorption following single high doses (500 mg/kg) was indicated by large amounts (50%) of radioactivity in the feces being associated with parent compound. For low- or highdose treatment, urinary excretion in female rats tended to be greater (up to 2-fold in low-dose rats) than that of male rats. Retention of dimethomorph or (14)C-dimethomorph-derived radioactivity was generally 1% for most tissues although the liver exhibited slightly higher levels (1.4%) and higher levels in the gastrointestinal tract organs were due to radioactivity in the lumenal contents.

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Metabolism / Metabolites
Rat Oral administration of dimethomorph (10 mg/kg single dose; 10 mg/kg 14-day repeated dose; 10 mg/kg 7-day repeated dose; 500 mg/kg single dose) results in rapid excretion into the urine and feces of rats. ... Urinary metabolites resulted from demethylation of the dimethoxyphenyl ring and oxidation of the morpholine ring. ...Biliary metabolites accounted for most of the fecal excretion following low-dose treatment. The major biliary metabolites were glucuronides of one and possibly two of the compounds produced by demethylation of the dimethoxyphenyl ring. The report provided a proposed metabolic pathway for dimethomorph.
In rats, the major route of metabolism is demethylation of one of the dimethoxy groups or by oxidation of one of the CH2 groups (ortho- or meta-position) of the morpholine ring.

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Biological Half-Life
Rat Oral administration of dimethomorph (10 mg/kg single dose; 10 mg/kg 14-day repeated dose; 10 mg/kg 7-day repeated dose; 500 mg/kg single dose) results in rapid excretion into the urine and feces of rats. ...Biliary excretion exhibited first-order kinetics with a lowdose (10 mg/kg) half-life of approximately three hours and a high-dose (500 mg/kg) half-life of 11 hours for males and about 6 hours for females.

[1]. Impact of Azoxystrobin, Dimethomorph, Fluazinam, Fosetyl-Al, and Metalaxyl on Growth, Sporulation, and Zoospore Cyst Germination of Three Phytophthora spp. Plant Dis. 2000 Apr;84(4):454-458.

[2]. Widely used pesticides with previously unknown endocrine activity revealed as in vitro antiandrogens. Environ Health Perspect. 2011 Jun;119(6):794-800.

[3]. Differential Activity of Carboxylic Acid Amide Fungicides Against Various Developmental Stages of Phytophthora infestans. Phytopathology. 2007 Oct;97(10):1274-83.

Dimethomorph is a mixture of (E)- and (Z)-dimethomorph in an unspecified ratio. It is used as a systemic fungicide used on vines, potatoes, and greenhouse crops; only the Z isomer has fungicidal activity. It has a role as a xenobiotic, an environmental contaminant and an antifungal agrochemical. It is a mixture and a morpholine fungicide. It contains an (E)-dimethomorph and a (Z)-dimethomorph.

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Mechanism of Action
Systemic fungicide with good protectant, curative and antisporulant activity. Inhibits the formation of the oomycete fungal cell wall. Only the Z-isomer is intrinsically active, but, because of rapid interconversion of isomers in the light, it has no advantage over the E-isomer in practice.

C21H22CLNO4

387.86

387.123

110488-70-5

Dimethomorph-d8;1346606-71-0

5889665

White to off-white solid powder

1.2±0.1 g/cm3

584.9±50.0 °C at 760 mmHg

125-149ºC

307.5±30.1 °C

0.0±1.6 mmHg at 25°C

1.581

3.71

48

0

4

5

27

512

0

COC1=C(C=C(C=C1)/C(=C/C(=O)N2CCOCC2)/C3=CC=C(C=C3)Cl)OC

QNBTYORWCCMPQP-NBVRZTHBSA-N

InChI=1S/C21H22ClNO4/c1-25-19-8-5-16(13-20(19)26-2)18(15-3-6-17(22)7-4-15)14-21(24)23-9-11-27-12-10-23/h3-8,13-14H,9-12H2,1-2H3/b18-14+

(E)-3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)-1-morpholin-4-ylprop-2-en-1-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : 6.67 mg/mL (17.20 mM)

配方 1 中的溶解度: ≥ 0.67 mg/mL (1.73 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 6.7 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 0.67 mg/mL (1.73 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 6.7mg/mL澄清的DMSO储备液加入到900μL 20％SBE-β-CD生理盐水中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。