DY131 (Synonyms: GSK 9089;DY-131;DY 131;GSK9089;GSK-9089) |
Catalog No.GC10394
One-Click Copy Product Info
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An ERRβ/γ agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 95167-41-2
Sample solution is provided at 25 µL, 10mM.
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IC50: N/A
DY131 is an agonist ligand for estrogen-related receptors ERRβ/γ. Estrogen receptor-related receptors (ERR) are orphan nuclear receptors constitutively activated without estrogen binding. ERRs may be involved in similar ER-mediated regulatory pathways and modulate estrogen responsiveness in certain target cells. The ERR subtypes, ERRβ/γ, are coexpressed in normal human prostatic epithelial cells and exhibit reduced expression in many prostate cancer cell lines.
In vitro: DY131 was evaluated for its selectivity and efficacy in modulating the transcriptional activity of ERRα/β/γ and ERβ/γ. CV-1 cells were transfected with reporter constructs or expression vectors and the fold activation of the reporter construct was determined at different concentrations of DY131. DY131 was found to be not able to activate the reporter construct or ERRα at any of the tested concentrations. In contrast, DY131 led to three- to fourfold activation of ERRβ at concentrations of 10-30 μM. Activity on ERRγ was more pronounced with five-fold activation at 3 μM and maximal 6.6-fold activity observed at 30 μM. Thus, DY131 was an selective ERRβ/γ ligand displaying preferential selectivity for ERRγ at lower concentrations [1].
In vivo: Currently, there is no animal in vivo data available for DY131 and its analogs.
Clinical trial: So far, no clinical study has been reported for DY131 and its analogs.
Reference:
[1] Yu DD,Forman BM. Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma. Bioorg Med Chem Lett.2005 Mar 1;15(5):1311-3.
| Cas No. | 95167-41-2 | SDF | |
| Sinónimos | GSK 9089;DY-131;DY 131;GSK9089;GSK-9089 | ||
| Chemical Name | N-[(E)-[4-(diethylamino)phenyl]methylideneamino]-4-hydroxybenzamide | ||
| Canonical SMILES | CCN(CC)C1=CC=C(C=C1)C=NNC(=O)C2=CC=C(C=C2)O | ||
| Formula | C18H21N3O2 | M.Wt | 311.38 |
| Solubility | ≥ 37.1 mg/mL in DMSO, ≥ 6.91 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2115 mL | 16.0576 mL | 32.1151 mL |
| 5 mM | 642.3 μL | 3.2115 mL | 6.423 mL |
| 10 mM | 321.2 μL | 1.6058 mL | 3.2115 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)