AZD-0284
Based on 3 publication(s) in Google Scholar
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.90%
- No. CAS: 2101291-07-8
- Fòrmula: C21H18F6N2O5S
- Peso molecular:524.43
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-12776
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HY-19770
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JNJ-61803534RORγt Inverse Agonist -
HY-119464
MRL-871RORγt Inverse Agonist -
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CintirorgonRORγ Agonist -
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SR0987RORγt Agonist -
HY-13421
SR1001RORα/γt Inverse Agonist -
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GNE-6468RORγ (RORc) Inverse Agonist -
HY-126037
(±)-ML 209RORγ Antagonist
Publications Citing Use of MedChemExpress (MCE) AZD-0284
More
Actividad biológica
Descripciòn
IC50 & Target
pIC50: 7.4 (FRET RORγ)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Thymocyte | IC50 |
229 nM
Compound: 20
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Apoptosis in C57BL/6NCrl mouse thymocytes assessed as survival incubated for 26 hrs by AnnexinV staining based by flow cytometry
Apoptosis in C57BL/6NCrl mouse thymocytes assessed as survival incubated for 26 hrs by AnnexinV staining based by flow cytometry
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[PMID: 34464130] |
In Vitro
AZD0284 (0.37 μM; 5 days) inhibits IL-17A production in human TH17 cells[1].
AZD0284 reduces polarization of TH17 into pathogenic TH17/1 cells. AZD0284 decreases frequency of single IL-17+cell as well as double positive TH17/1 cells. AZD0284 reduces IL-17A secretion and RNA expression of IL-17A, IL-17F, IL-22 and IL-23R[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2101291-07-8
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Appearance Solid
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Peso molecular 524.43
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Fòrmula C21H18F6N2O5S
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Color White to off-white
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SMILES
O=C([C@@H]1N(C(C)=O)CC2=C1C=CC(S(=O)(C)=O)=C2)NC3=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Oct;300(10):107765. PMID: 39276936 -
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Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (190.68 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 0.83 mg/mL (1.58 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.58 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Protocolo
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Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.
Pureza y Documentación
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Ficha de datos (280 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
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9068 mL | 9.5342 mL | 19.0683 mL | 47.6708 mL |
| 5 mM | 0.3814 mL | 1.9068 mL | 3.8137 mL | 9.5342 mL | |
| 10 mM | 0.1907 mL | 0.9534 mL | 1.9068 mL | 4.7671 mL | |
| 15 mM | 0.1271 mL | 0.6356 mL | 1.2712 mL | 3.1781 mL | |
| 20 mM | 0.0953 mL | 0.4767 mL | 0.9534 mL | 2.3835 mL | |
| 25 mM | 0.0763 mL | 0.3814 mL | 0.7627 mL | 1.9068 mL | |
| 30 mM | 0.0636 mL | 0.3178 mL | 0.6356 mL | 1.5890 mL | |
| 40 mM | 0.0477 mL | 0.2384 mL | 0.4767 mL | 1.1918 mL | |
| 50 mM | 0.0381 mL | 0.1907 mL | 0.3814 mL | 0.9534 mL | |
| 60 mM | 0.0318 mL | 0.1589 mL | 0.3178 mL | 0.7945 mL | |
| 80 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5959 mL | |
| 100 mM | 0.0191 mL | 0.0953 mL | 0.1907 mL | 0.4767 mL |
AZD-0284 Related Classifications
HY-120384 Related Classifications
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