Dimethomorph has EC50s of less than 0.1 µg/mL, 0.14 µg/mL, and 0.38 µg/mL for Phytophthora capsici, P. citrophthora, and P. parasitica, respectively, inhibiting these oomycetes [1]. Although dimethomorph does not reduce AR activity in a yeast anti-androgen screen (IC50s = 0.263 and 38.5 µM), it does so in a reporter assay on MDA-kb2 human breast cancer cells [2].

Absorption, Distribution and Excretion
Following oral administration of dimethomorphine to rats (single dose 10 mg/kg; repeated administration of 10 mg/kg for 14 days; repeated administration of 10 mg/kg for 7 days; single dose 500 mg/kg), the drug was rapidly excreted in urine and feces. In all dosing regimens, the majority (80-90%) of the radiolabeled material was excreted in feces. A small amount (6-16%) was excreted in urine, while only trace amounts (0.1-0.4%) were detected in organs and tissues. The rapid excretion of metabolites in urine and bile indicates rapid drug absorption. After a single high-dose administration (500 mg/kg), a large amount (50%) of the radioactive material in the feces bound to the parent compound, indicating that absorption had reached saturation. Regardless of whether the treatment was low or high dose, urinary excretion was often higher in female rats than in male rats (up to 2 times in the low-dose group). The retention rate of dimethmorphine or radioactive substances derived from 14C-dimethmorphine in most tissues is typically 1%, but the retention rate in the liver is slightly higher (1.4%), while the higher retention rate in gastrointestinal organs is attributed to radioactivity in the luminal contents. Metabolites/Metabolites: Following oral administration of dimethmorphine to rats (single dose 10 mg/kg; repeated doses over 14 days; repeated doses over 7 days; single dose 500 mg/kg), the drug is rapidly excreted in urine and feces. …Urinary metabolites originate from the demethylation of the dimethoxybenzene ring and the oxidation of the morpholine ring. After low-dose treatment, bile metabolites account for the majority of fecal excretion. The main bile metabolite is one (or possibly two) glucuronide from the demethylation of the dimethoxybenzene ring. This report presents the metabolic pathway of dimethmorphine. In rats, the primary metabolic pathway is demethylation of the dimethoxy group or oxidation of the CH2 group (ortho- or meta-) on the morphine ring.
Biological Half-Life
Following oral administration of dimethmorphine to rats (10 mg/kg single dose; 10 mg/kg repeated doses over 14 days; 10 mg/kg repeated doses over 7 days; 500 mg/kg single dose), the drug is rapidly excreted in urine and feces. Bile excretion exhibits first-order kinetics, with a half-life of approximately 3 hours for low doses (10 mg/kg) and approximately 11 hours for males and approximately 6 hours for females for high doses (500 mg/kg).

[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.

Dimethylmorpholine is a mixture of (E)-dimethylmorpholine and (Z)-dimethylmorpholine, with no specific ratio specified. It is a systemic fungicide used on grapevines, potatoes, and greenhouse crops; only the Z isomer has fungicidal activity. It is both an exogenous substance and an environmental pollutant and antifungal pesticide. It is a mixture and a morpholine fungicide. It contains (E)-dimethylmorpholine and (Z)-dimethylmorpholine. Mechanism of Action: A systemic fungicide with good protective, curative, and antispore activities. Inhibits oomycete cell wall formation. Only the Z isomer itself is active, but because the isomers rapidly interconvert under light, it is not more advantageous than the E isomer in practical applications.

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

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

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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)

Solubility in Formulation 1: ≥ 0.67 mg/mL (1.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 0.67 mg/mL (1.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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 (Please use freshly prepared in vivo formulations for optimal results.)