CC618
Based on 1 Customer Validation
CC618 is a selective PPARβ/δ antagonist. CC618 covalently modifies conserved Cys249 in the PPARβ/δ ligand-binding pocket via nucleophilic aromatic substitution, converting its thiol moiety to a 5-trifluoromethyl-2-pyridylthioether.
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- Reinheit: 99.94%
- CAS. Nr.: 1680204-90-3
- Formel: C20H15F6N3O3S2
- Molecular Weight:523.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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PPARδ 10 μM (IC50) |
PPARβ |
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Cell Line
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Type | Value | Description | References |
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| COS-1 | IC50 |
10 μM
Compound: 10a, CC618
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Antagonist activity against pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as inhibition of GW501516-induced receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
Antagonist activity against pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as inhibition of GW501516-induced receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
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[PMID: 25768705] |
CC618 (dilution series; 19 h) selectively antagonizes agonist-induced PPARδ activity in Cos-1 cells with an IC50 of 10.0 μM, with minimal activity against PPARα and PPARγ subtypes[1].
CC618 (10 μM; 15 min) covalently modifies the Cys249 residue within the ligand-binding pocket of purified human PPARδ protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1680204-90-3
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Appearance Solid
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Molecular Weight 523.47
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Formel C20H15F6N3O3S2
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Color White to off-white
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SMILES
O=C(NCCS(=O)(C1=NC=C(C=C1)C(F)(F)F)=O)C2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C
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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 : ≥ 25 mg/mL (47.76 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.
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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 1.9103 mL | 9.5516 mL | 19.1033 mL | 47.7582 mL |
| 5 mM | 0.3821 mL | 1.9103 mL | 3.8207 mL | 9.5516 mL | |
| 10 mM | 0.1910 mL | 0.9552 mL | 1.9103 mL | 4.7758 mL | |
| 15 mM | 0.1274 mL | 0.6368 mL | 1.2736 mL | 3.1839 mL | |
| 20 mM | 0.0955 mL | 0.4776 mL | 0.9552 mL | 2.3879 mL | |
| 25 mM | 0.0764 mL | 0.3821 mL | 0.7641 mL | 1.9103 mL | |
| 30 mM | 0.0637 mL | 0.3184 mL | 0.6368 mL | 1.5919 mL | |
| 40 mM | 0.0478 mL | 0.2388 mL | 0.4776 mL | 1.1940 mL |
CC618 Related Classifications
HY-120188 Related Classifications
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