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ARN5187

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Catalog No. T61883Cas No. 1287451-26-6

ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis.

ARN5187

ARN5187

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Catalog No. T61883Cas No. 1287451-26-6
ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,5206-8 weeks6-8 weeks
50 mg$1,9806-8 weeks6-8 weeks
100 mg$2,5006-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis.
In vitro
ARN5187 (compound 1) (0-100 μM; 48 h) demonstrates cytotoxicity with an EC50 of 23.5 μM in BT-474 cells and IC50 values of 30.14 μM and >100 μM in BT-474 and HMEC cells, respectively [1][2]. In HEK-293 cells, ARN5187 (0-100 μM) activates the RevRE reporter in a concentration-dependent manner [1]. ARN5187 (25, 50 μM) exhibits lysosomotropic-independent REV-ERB antagonistic activity [1], and at 50 μM (24 h), it shows autophagy inhibition and affects autophagy formation and maturation [1]. In BT-474 cells, ARN5187 significantly enhances the expression of BMAL1, PER1, and PEPCK in a dose-dependent manner (25, 50 μM), and at 50 μM (24 h), significantly increases the expression of α-LC3-II, α-p62, and α-Cleaved PARP [1].
Chemical Properties
Molecular Weight397.53
FormulaC24H32FN3O
Cas No.1287451-26-6
SmilesN(CC1=CC(CN2CCN(C)CC2)=C(O)C=C1)C3(CCCC3)C4=C(F)C=CC=C4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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