ZK 216348
Based on 1 Customer Validation
ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.
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- Pureté: 99.93%
- CAS No.: 669073-68-1
- Formule: C24H23F3N2O5
- Masse moléculaire:476.45
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
>2000 nM
Compound: 2a, ZK-216348
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Activation of MMTV in HeLa cells measured by luciferase activity
Activation of MMTV in HeLa cells measured by luciferase activity
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[PMID: 17181172] |
| HFF | EC50 |
91 nM
Compound: 2a, ZK-216348
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Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
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[PMID: 17181172] |
| HFF | IC50 |
59 nM
Compound: 2a, ZK-216348
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Inhibition of IL1-stimulated IL6 production in HFF cells
Inhibition of IL1-stimulated IL6 production in HFF cells
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[PMID: 17181172] |
In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC50 of 89 nM and 52 nM, respectively[1].
Participation of an active GR in the antiinflammatory response of ZK 216348 is further investigated in Caco-2 cells, where the TNF-α-induced expression of the proinflammatory cytokine IL-8 is suppressed in the presence of ZK 216348[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI mice (26-28 g) and Wistar rats (140-160 g) injection with Croton oil[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg and 30 mg/kg
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Administration:Subcutaneous injection; for 24 hours
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Result:Inhibited ear edema in mice and rats.
Chemical Information
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CAS No. 669073-68-1
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Appearance Solid
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Masse moléculaire 476.45
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Formule C24H23F3N2O5
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Color White to off-white
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SMILES
O=C1C2=CC=C(C=C2C(C)=NO1)NC(C(C(F)(F)F)(O)CC(C)(C3=C4C(CCO4)=CC=C3)C)=O
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Synonyms
(+)-ZK 216348
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : ≥ 200 mg/mL (419.77 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Schäcke H, et al. Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc Natl Acad Sci U S A. 2004 Jan 6;101(1):227-32. [Content Brief]
[2]. Reuter KC, et al. Selective glucocorticoid receptor agonists for the treatment of inflammatory bowel disease: studies in mice with acute trinitrobenzene sulfonic acid colitis. J Pharmacol Exp Ther. 2012 Apr;341(1):68-80. [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 (sealed storage, away from moisture and light). 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 | 2.0989 mL | 10.4943 mL | 20.9886 mL | 52.4714 mL |
| 5 mM | 0.4198 mL | 2.0989 mL | 4.1977 mL | 10.4943 mL | |
| 10 mM | 0.2099 mL | 1.0494 mL | 2.0989 mL | 5.2471 mL | |
| 15 mM | 0.1399 mL | 0.6996 mL | 1.3992 mL | 3.4981 mL | |
| 20 mM | 0.1049 mL | 0.5247 mL | 1.0494 mL | 2.6236 mL | |
| 25 mM | 0.0840 mL | 0.4198 mL | 0.8395 mL | 2.0989 mL | |
| 30 mM | 0.0700 mL | 0.3498 mL | 0.6996 mL | 1.7490 mL | |
| 40 mM | 0.0525 mL | 0.2624 mL | 0.5247 mL | 1.3118 mL | |
| 50 mM | 0.0420 mL | 0.2099 mL | 0.4198 mL | 1.0494 mL | |
| 60 mM | 0.0350 mL | 0.1749 mL | 0.3498 mL | 0.8745 mL | |
| 80 mM | 0.0262 mL | 0.1312 mL | 0.2624 mL | 0.6559 mL | |
| 100 mM | 0.0210 mL | 0.1049 mL | 0.2099 mL | 0.5247 mL |
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