DY131 Estrogen/progestogen Receptor activator

Cat.No.S5364

DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
DY131 Estrogen/progestogen Receptor activator Chemical Structure

Chemical Structure

Molecular Weight: 311.38

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 311.38 Formula

C18H21N3O2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 95167-41-2 -- Storage of Stock Solutions

Synonyms N/A Smiles CCN(CC)C1=CC=C(C=C1)C=NNC(=O)C2=CC=C(C=C2)O

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (199.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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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.

Mechanism of Action

Targets/IC50/Ki
ERRβ [1]
ERRγ [1]
In vitro
DY131 is an ERRβ/γ-specific ligand that displays preferential selectivity for ERRγ at lower concentrations. It has no activity on the related receptors ERRα, ERα and ERβ[1]. This compound inhibits growth in a diverse panel of breast cancer cell lines, causing cell death that involves the p38 stress kinase pathway and a bimodal cell cycle arrest. ERRβ2 facilitates the block in G2/M, and this chemical delays progression from prophase to anaphase. ERRβ2 is a cytosolic protein that also localizes to centrosomes, and this treatment leads to the appearance of multi- and monopolar spindles, thus causes mitotic spindle defects[2].
References

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