AR7 Retinoid Receptor inhibitor

AR7 is a retinoic acid receptor α (RARα) antagonist. This compound is a potent and selective inhibitor of RARα, demonstrating high affinity and specificity for this receptor subtype. It effectively blocks the binding of retinoic acid to RARα, thereby inhibiting downstream signaling pathways. In cellular assays, this chemical has been shown to suppress the proliferation of various cancer cell lines that are dependent on RARα signaling. Additionally, it induces apoptosis in these cells, highlighting its potential as a therapeutic agent. The pharmacological profile of this antagonist supports its use in studying RARα-mediated processes and in developing treatments for related diseases.

AR7 Retinoid Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 257.71

Purity & Quality Control

Batch: S660501 DMSO]4 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.87%
99.87

Related Products

Mechanism of Action

In vitro

In vitro

AR7 significantly activates CMA activity in mouse fibroblasts. A marked increase in CMA-activating potency is found when this compound and GR1 are combined, supporting their cooperative effect. Treatment with the transcriptional repressor Actinomycin D partially reduces the stimulatory effect of this chemical on CMA, consistent with transcriptional changes contributing to the upregulation of CMA.[1]

Cell Research Cell lines Mouse fibroblasts
Concentrations 0-10 μM, 20μM
Incubation Time 16 h
Method

Mouse fibroblasts expressing the KFERQ-mcherry1 photoactivable reporter with or without AR7 (20μM) imaged 16 h after photoactivation.

In Vivo

In vivo

Reactivation of CMA by treatment with AR7 inhibits diclofenac-induced lipid accumulation and hepatotoxicity. [2]

References

  • https://pubmed.ncbi.nlm.nih.gov/23584676/

Chemical Information

Molecular Weight 257.71 Formula

C15H12ClNO

CAS No. 80306-38-3 SDF --
Synonyms N/A
Smiles CC1=CC=C(C=C1)C2=NC3=C(C=C(C=C3)Cl)OC2

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 4 mg/mL ( (15.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.