GNE-3500
Based on 1 Customer Validation
GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.90%
- CAS. Nr.: 1537859-24-7
- Formel: C24H30FN3O3S
- Molecular Weight:459.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Biologische Aktivität
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ROR-γ 12 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.047 μM
Compound: 2
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Inverse agonist activity at GAL4-fused human RORc expressed in HEK293 cells assessed as activation of basal transcriptional activity by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORc expressed in HEK293 cells assessed as activation of basal transcriptional activity by dual-glo luciferase reporter gene assay
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[PMID: 27524313] |
| HEK293 | EC50 |
5.4 μM
Compound: 2
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Inverse agonist activity at GAL4-fused human RORa expressed in HEK293 cells assessed as activation of basal transcriptional activity by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORa expressed in HEK293 cells assessed as activation of basal transcriptional activity by dual-glo luciferase reporter gene assay
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[PMID: 27524313] |
| HEK293 | EC50 |
5.4 μM
Compound: 2
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Inverse agonist activity at GAL4-fused human RORb expressed in HEK293 cells assessed as activation of basal transcriptional activity by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORb expressed in HEK293 cells assessed as activation of basal transcriptional activity by dual-glo luciferase reporter gene assay
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[PMID: 27524313] |
| PBMC | EC50 |
>20 μM
Compound: 2
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Cytotoxicity against human PBMC assessed as cell viability measured after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human PBMC assessed as cell viability measured after 48 hrs by CellTiter-Glo assay
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[PMID: 27524313] |
| PBMC | EC50 |
>20 μM
Compound: 2
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Inhibition of IFN-gamma production in anti-CD3 and anti-CD28 stimulated human PBMC measured after 1 hr by Sandwich ELISA
Inhibition of IFN-gamma production in anti-CD3 and anti-CD28 stimulated human PBMC measured after 1 hr by Sandwich ELISA
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[PMID: 27524313] |
| PBMC | EC50 |
0.45 μM
Compound: 2
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Inhibition of IL-17AA production in anti-CD3 and anti-CD28 stimulated human PBMC measured after 1 hr by Sandwich ELISA
Inhibition of IL-17AA production in anti-CD3 and anti-CD28 stimulated human PBMC measured after 1 hr by Sandwich ELISA
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[PMID: 27524313] |
Chemical Information
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CAS. Nr. 1537859-24-7
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Appearance Solid
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Molecular Weight 459.58
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Formel C24H30FN3O3S
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Color White to off-white
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SMILES
FC1=CC(N2CCN(C(C)=O)CC2)=CC=C1CN3[C@@H](C)CC[C@H](C4=CC=CC=C4)S3(=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (108.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1.25 mg/mL (2.72 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.72 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Reinheit & Dokumentation
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Data Sheet (272 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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Handling Instructions (2659 KB)
Verweise
[1]. Fauber BP, et al., Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist. J Med Chem. 2015 Jul 9;58(13):5308-22. [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, 6 months; -20°C, 1 month. 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 | 2.1759 mL | 10.8795 mL | 21.7590 mL | 54.3975 mL |
| 5 mM | 0.4352 mL | 2.1759 mL | 4.3518 mL | 10.8795 mL | |
| 10 mM | 0.2176 mL | 1.0879 mL | 2.1759 mL | 5.4397 mL | |
| 15 mM | 0.1451 mL | 0.7253 mL | 1.4506 mL | 3.6265 mL | |
| 20 mM | 0.1088 mL | 0.5440 mL | 1.0879 mL | 2.7199 mL | |
| 25 mM | 0.0870 mL | 0.4352 mL | 0.8704 mL | 2.1759 mL | |
| 30 mM | 0.0725 mL | 0.3626 mL | 0.7253 mL | 1.8132 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5440 mL | 1.3599 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.0879 mL | |
| 60 mM | 0.0363 mL | 0.1813 mL | 0.3626 mL | 0.9066 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6800 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5440 mL |
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