DY131
Based on 3 publication(s) in Google Scholar
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.
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- Pureza: 99.22%
- No. CAS: 95167-41-2
- Fòrmula: C18H21N3O2
- Peso molecular:311.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DY131
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Actividad biológica
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ERRγ |
ERRβ |
DY131 (0.1-30 μM; 5 days) treatment suppresses cell proliferation and reduces BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner, with higher suppression in LNCaP-ERRγ clone[1].
DY131inhibits Shh induced accumulation of Smo::EGFP with an IC50 of 0.8 μM. DY131 suppresses SAG (100 nM) induced accumulation of Smo::EGFP in the primary cilium and Gli transcription activity with an IC50 of ~2 μM[3].
DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh[3].
A selective ERRγ agonist, DY131, inhibits the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP-ERRγ and LNCaP cells
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Concentration:0.1 μM, 1 μM, 10 μM, 30 μM
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Incubation Time:5 days
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Result:Suppressed cell proliferation and reduced BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mature male mice (C57BL/6) (8-10 week-old; ~24.3 g)[5]
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Dosage:5 μg/kg
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Administration:Subcutaneous injection; every second day; for 12 days
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Result:Increased P450scc, StAR and HMGCR while decreased HSL expressions.
Chemical Information
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No. CAS 95167-41-2
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Appearance Solid
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Peso molecular 311.38
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Fòrmula C18H21N3O2
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Color Light yellow to green yellow
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SMILES
O=C(N/N=C/C1=CC=C(N(CC)CC)C=C1)C2=CC=C(O)C=C2
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Synonyms
GSK 9089
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Transl Med
ESRRG-PKM2 axis reprograms metabolism to suppress esophageal squamous carcinoma progression and enhance anti-PD-1 therapy efficacy. [Abstract]2023 Sep 7;21(1):605. PMID: 37679788 -
Front Pharmacol
Estrogen-Related Receptor γ Agonist DY131 Ameliorates Lipopolysaccharide-Induced Acute Liver Injury. [Abstract]2021 Apr 23:12:626166. PMID: 33967760 -
Solvente y solubilidad
DMSO : 50 mg/mL (160.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.03 mM); 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.03 mM); 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yu S, et al. ERRgamma suppresses cell proliferation and tumor growth of androgen-sensitive and androgen-insensitive prostate cancer cells and its implication as a therapeutic target for prostate cancer. Cancer Res. 2007;67(10):4904-14. [Content Brief]
[2]. Donna D. Yu, Barry Marc Forman. Identification of an agonist ligand for estrogen-related receptors ERRβ/γ. Bioorganic & Medicinal Chemistry Letters. 2005,15(5): 1311-1313. [Content Brief]
[3]. Wang Y, et al. Selective identification of hedgehog pathway antagonists by direct analysis of smoothened ciliary translocation . ACS Chem Biol. 2012,15;7(6):1040-8. [Content Brief]
[4]. Yamamoto T, et al. Estrogen-related receptor-γ regulates estrogen receptor-α responsiveness in uterine endometrial cancer. Int J Gynecol Cancer. 2012;22(9):1509-16. [Content Brief]
[5]. A Pacwa, et al. Interplay between estrogen-related receptors and steroidogenesis-controlling molecules in adrenals. In vivo and in vitro study. Acta Histochem. 2018 Jul;120(5):456-467. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2115 mL | 16.0576 mL | 32.1151 mL | 80.2878 mL |
| 5 mM | 0.6423 mL | 3.2115 mL | 6.4230 mL | 16.0576 mL | |
| 10 mM | 0.3212 mL | 1.6058 mL | 3.2115 mL | 8.0288 mL | |
| 15 mM | 0.2141 mL | 1.0705 mL | 2.1410 mL | 5.3525 mL | |
| 20 mM | 0.1606 mL | 0.8029 mL | 1.6058 mL | 4.0144 mL | |
| 25 mM | 0.1285 mL | 0.6423 mL | 1.2846 mL | 3.2115 mL | |
| 30 mM | 0.1071 mL | 0.5353 mL | 1.0705 mL | 2.6763 mL | |
| 40 mM | 0.0803 mL | 0.4014 mL | 0.8029 mL | 2.0072 mL | |
| 50 mM | 0.0642 mL | 0.3212 mL | 0.6423 mL | 1.6058 mL | |
| 60 mM | 0.0535 mL | 0.2676 mL | 0.5353 mL | 1.3381 mL | |
| 80 mM | 0.0401 mL | 0.2007 mL | 0.4014 mL | 1.0036 mL | |
| 100 mM | 0.0321 mL | 0.1606 mL | 0.3212 mL | 0.8029 mL |
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