1. Metabolic Enzyme/Protease
  2. Herbicide
  3. Epyrifenacil

Epyrifenacil is a protoporphyrinogen oxidase (PPO) inhibiting herbicide, potently targeting the PPO2 isoform from weeds such as Amaranthus palmeri with an IC50 of 0.637 nM. Epyrifenacil also inhibits liver mitochondrial PPO across species, with IC50 values of 2.2 nM (mouse), 2.6 nM (rat), 12.1 nM (rabbit), 7.6 nM (dog), and 10.2 nM (human). Epyrifenacil induces liver tumor development in mice. Epyrifenacil can be used for weed control, and also used as a tool compound in toxicological research to study the mechanism of PPO inhibition, chemical-induced hepatotoxicity, and the mode of action of non-genotoxic carcinogens in rodents[3].

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Epyrifenacil

Epyrifenacil 構造式

CAS 番号 : 353292-31-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 511 在庫あり
Solution
10 mM * 1 mL in DMSO USD 511 在庫あり
Solid
5 mg $449 在庫あり
10 mg $718 在庫あり
25 mg $1437 在庫あり
50 mg $2300 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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製品説明

Epyrifenacil is a protoporphyrinogen oxidase (PPO) inhibiting herbicide, potently targeting the PPO2 isoform from weeds such as Amaranthus palmeri with an IC50 of 0.637 nM. Epyrifenacil also inhibits liver mitochondrial PPO across species, with IC50 values of 2.2 nM (mouse), 2.6 nM (rat), 12.1 nM (rabbit), 7.6 nM (dog), and 10.2 nM (human). Epyrifenacil induces liver tumor development in mice. Epyrifenacil can be used for weed control, and also used as a tool compound in toxicological research to study the mechanism of PPO inhibition, chemical-induced hepatotoxicity, and the mode of action of non-genotoxic carcinogens in rodents[1][2][3].

体外実験

Epyrifenacil (156-5000 μg/plate) shows no genotoxic potential in the bacterial reverse mutation test[2].
Epyrifenacil (1.9-120.0 μg/mL) shows no genotoxic potential in the mammalian cell gene mutation test[2].
Epyrifenacil (15.6-125 μg/mL) shows no genotoxic potential in the mammalian chromosomal aberration test[2].
Epyrifenacil (40 ppm) exhibits systemic herbicidal activity in three-leaf stage wild soybean plants, completely killing whole plants including shoot apical meristems within 5 days of foliar application at 40 ppm[3].
Epyrifenacil (20 g a.i. ha-1) provides complete control of barnyardgrass and Italian ryegrass in glasshouse pot trials when applied as a late-post foliar spray at 20 g a.i. ha-1[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Epyrifenacil (5, 25, and 100 ppm; dietary; ad libitum daily; 90 days) induces dose-dependent hepatotoxicity and anemia in Crl:CD1(ICR) mice, with NOAELs of 0.7 mg/kg bw/day for males and 4.1 mg/kg bw/day for females[1].
Epyrifenacil (50, 300, and 800 ppm; dietary; ad libitum daily; 90 days) induces dose-dependent hepatotoxicity and anemia in Crl:CD(SD) rats, with NOAELs of 3 mg/kg bw/day for males and 19 mg/kg bw/day for females[1].
Epyrifenacil (100, 300, and 1000 mg/kg; p.o.; daily; 90 days) induces dose-dependent anemia and liver glycogen elevation in TOYO beagles, with NOAELs of 100 mg/kg bw/day for males and 300 mg/kg bw/day for females, and no evident hepatocyte injury[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Crl:CD1(ICR) mice[1]
Dosage: 5; 25; 100 ppm
Administration: dietary; ad libitum daily; 90 days
Result: Induced hepatocyte injury characterized by hepatocellular degeneration/necrosis and/or single-cell necrosis/apoptosis, hepatocellular hypertrophy, and anemia.
Exhibited NOAEL of 0.7 mg/kg bw/day for males and 4.1 mg/kg bw/day for females.
Animal Model: Crl:CD(SD) rats[1]
Dosage: 50; 300; 800 ppm
Administration: dietary; ad libitum daily; 90 days
Result: Induced hepatocyte injury characterized by hepatocellular degeneration/necrosis and/or single-cell necrosis/apoptosis, hepatocellular hypertrophy, and anemia.
Exhibited NOAEL of 3 mg/kg bw/day for males and 19 mg/kg bw/day for females.
Animal Model: TOYO dogs[1]
Dosage: 100; 300; 1000 mg/kg/day
Administration: p.o.; daily; 90 days
Result: Induced anemia and increased liver glycogen associated with increased alkaline phosphatase (ALP), with no evident hepatocyte injury.
Exhibited NOAEL of 100 mg/kg bw/day for males and 300 mg/kg bw/day for females.
分子量

517.81

分子式

C21H16ClF4N3O6

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC(C(N(C)C1=O)=CC(N1C2=C(F)C=C(Cl)C(OC3=CC=CN=C3OCC(OCC)=O)=C2)=O)(F)F

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (193.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9312 mL 9.6561 mL 19.3121 mL
5 mM 0.3862 mL 1.9312 mL 3.8624 mL
10 mM 0.1931 mL 0.9656 mL 1.9312 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

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体積 (開始)

V1

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9312 mL 9.6561 mL 19.3121 mL 48.2803 mL
5 mM 0.3862 mL 1.9312 mL 3.8624 mL 9.6561 mL
10 mM 0.1931 mL 0.9656 mL 1.9312 mL 4.8280 mL
15 mM 0.1287 mL 0.6437 mL 1.2875 mL 3.2187 mL
20 mM 0.0966 mL 0.4828 mL 0.9656 mL 2.4140 mL
25 mM 0.0772 mL 0.3862 mL 0.7725 mL 1.9312 mL
30 mM 0.0644 mL 0.3219 mL 0.6437 mL 1.6093 mL
40 mM 0.0483 mL 0.2414 mL 0.4828 mL 1.2070 mL
50 mM 0.0386 mL 0.1931 mL 0.3862 mL 0.9656 mL
60 mM 0.0322 mL 0.1609 mL 0.3219 mL 0.8047 mL
80 mM 0.0241 mL 0.1207 mL 0.2414 mL 0.6035 mL
100 mM 0.0193 mL 0.0966 mL 0.1931 mL 0.4828 mL
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Epyrifenacil
製品番号:
HY-139838
数量:
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