製品番号: HY-12643

エプリノメクチン

(別名: Eprinomectin; MK-397)

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Based on 1 Customer Validation

Eprinomectin (MK-397) is a type of avermectin. Eprinomectin, as a broad-spectrum fungicide, has insecticidal, insecticidal and acaricidal activities. Eprinomectin induces apoptosis and autophagy in prostate cancer cells and has antitumor activity.

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純度: 98.02%
CAS 番号: 123997-26-2

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Eprinomectin 構造式

CAS 番号: 123997-26-2

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価格（税別）

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数量

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

Mite

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体外実験

Eprinomectin (2.5-50 μM; 0-48 h) significantly inhibits DU145 cell viability (IC₅₀: 12.5 µM), colony formation and migration ability, and induces G0/G1 phase cell cycle arrest^[1].
Eprinomectin (10-50 μM; 48 h) induces apoptosis and autophagy, increases the production of reactive oxygen species and endoplasmic reticulum stress, and promotes β-catenin nucleoplasmic translocation in DU145 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

DU145 cells
Concentration:

2.5, 5, 10, 25 and 50 μM
Incubation Time:

48 h
Result:

Significantly inhibited the cell viability.

Western Blot Analysis^[1]

Cell Line:

DU145 cells
Concentration:

10, 25 and 50 μM
Incubation Time:

48 h
Result:

Promoted the protein expression of the pro-apoptotic marker BAD and DNA damage marker pH2AX as well as caspase-9 in a concentration-dependent manner.
Inhibited DNA repair by decreasing PARP-1.

体内実験

Eprinomectin (0.08-0.5 mg/kg; Local pipette delivery; 14 days) has insecticidal, insecticidal and acaricidal activities in cattle^[2].
Pharmacokinetic Analysis in cattle^[1]

Route	Dose (μg/kg)	K_el (day^-1)	t_1/2 (day)	T_max (day)	C_max (ng/mL)	AUC_0-t (ng day mL^-1)	AUC_0-∞ (ng day mL^-1)	AUC_0-t/AUC_0-∞
s.c.	200	0.267	2.959	1.333	47.15	228.08	240.50	0.947

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

Animal Model:

Infective nematode or chorioptes bovis treated male Jersey calves^[2]
Dosage:

0.08, 0.16, 0.2, 0.24 and 0.5mg/kg
Administration:

Delivered topically from the tailhead to the withers at skin level via a pipette; 14 days
Result:

Produced maximal or near maximal efficacy against most of the adult endoparasites with the exception of T. colubriformis (87%) and C. oncophora (88%) at lowest dosage (0.08 mg/kg).
Produced ≥ 95% control at all dosage levels by day 14 post-treatment and was maintained at or near this efficacious level for the 6-week duration of the trial.

化学情報

CAS 番号 123997-26-2
性状 Solid
Color White to off-white
SMILES

CC(C)C.O[C@]1([C@](C=C2C)([H])C(O[C@]3([H])C[C@](O[C@H]([R])[C@H]4C)(C=C4)O[C@@](C/C=C5\C)([H])C3)=O)[C@]([C@@H]2O)([H])OC/C1=C\C=C\[C@@H]([C@@H]5O[C@H](O[C@H]6C)C[C@@H]([C@H]6O[C@H](O[C@H]7C)C[C@@H]([C@@H]7NC(C)=O)OC)OC)C.CC(C)CC.[B1a].[B1b]
別名

Eprinomectin; MK-397
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 125 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

体内:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL; Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL; 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Samy A, et al. Eprinomectin: a derivative of ivermectin suppresses growth and metastatic phenotypes of prostate cancer cells by targeting the β-catenin signaling pathway. J Cancer Res Clin Oncol. 2023 Sep;149(11):9085-9104. [Content Brief]

[2]. Shoop WL, et al. Eprinomectin: a novel avermectin for use as a topical endectocide for cattle. Int J Parasitol. 1996 Nov;26(11):1237-42. [Content Brief]

[3]. do Nascimento CG, et al. Injectable eprinomectin for cattle: Tick efficacy and pharmacokinetics. J Vet Pharmacol Ther. 2020 Mar;43(2):171-178. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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