ZK756326 dihydrochloride
Based on 1 publication(s) in Google Scholar
ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1780259-94-0
- Formula: C21H30Cl2N2O3
- Molecular Weight:429.38
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ZK756326 dihydrochloride
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Biological Activity
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CCR8 1.8 μM (IC50, in U87 cells) |
5-HT2B 4.4 μM (IC50) |
5-HT1A 5.4 μM (IC50) |
5-HT6 5.9 μM (IC50) |
5-HT5A 16 μM (IC50) |
5-HT2C 34.8 μM (IC50) |
α2A <20 μM (IC50) |
ZK 756326 inhibits the binding of the CCR8 ligand I-309 (CCL1), with an IC50 value of 1.8 μM. ZK 756326 is a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. ZK 756326 stimulates extracellular acidification in cells expressing human CCR8. Binding competition assays are performed on a series of other G-protein-coupled receptors to determine whether the interaction of ZK 756326 is specific for CCR8. In these assays, ZK 756326 is tested at 50 μM for inhibition of radiolabeled ligand binding. At this concentration, ZK 756326 shows >28 fold specificity for CCR8 compared with 26 other GPCRs, all with IC50 values of >50 μM. There is less selectivity when ZK 756326 is tested against the serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and the adrenergic receptor α2A, in which IC50 values of 5.4, 4,4, 34.8, 16, 5.9, and <20 μM (at 20 μM 65% inhibition), respectively, are observed. The compound is unlikely to be an agonist on these biogenic amine receptors, because when tested at concentrations up to 10 μM on a representative receptor, 5-HT1A, it shows no agonist activity in a GTPγS binding assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1780259-94-0
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Appearance Solid
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Molecular Weight 429.38
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Formula C21H30Cl2N2O3
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Color White to off-white
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SMILES
OCCOCCN1CCN(CC2=CC=CC(OC3=CC=CC=C3)=C2)CC1.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Biological characterization of ligands targeting the human CC chemokine receptor 8 (CCR8) reveals the biased signaling properties of small molecule agonists. [Abstract]2021 Jun:188:114565. PMID: 33872569
Solvent & Solubility
H2O : 50 mg/mL (116.45 mM; Need ultrasonic)
DMSO : 27.5 mg/mL (64.05 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.75 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (116.45 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
U87 MG cells expressing CCR8 are plated on poly-D-lysine-coated black 96-well plates at 10,000 cells/well and are cultured overnight. Cells are then loaded with Calcium 3, a Ca2+-sensitive non-wash fluorescence dye, for 60 min at 37°C in Hanks' balanced salts solution containing 20 mM HEPES, 3.2 mM CaCl2, 1% (v/v) fetal bovine serum, and 2.5 mM probenecid. Changes in intracellular free-Ca2+ concentration are measured with Fluorometric Imaging Plate Reader (FLIPR 3) immediately after the addition of agonist at room temperature. Cross-desensitization experiments are performed by a first addition of the agonist (CCL1 at 30 nM or ZK 756326 at 3 μM), immediately followed by a second addition of 100 nM CCL1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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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)
References
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). 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 / H2O | 1 mM | 2.3289 mL | 11.6447 mL | 23.2894 mL | 58.2235 mL |
| 5 mM | 0.4658 mL | 2.3289 mL | 4.6579 mL | 11.6447 mL | |
| 10 mM | 0.2329 mL | 1.1645 mL | 2.3289 mL | 5.8223 mL | |
| 15 mM | 0.1553 mL | 0.7763 mL | 1.5526 mL | 3.8816 mL | |
| 20 mM | 0.1164 mL | 0.5822 mL | 1.1645 mL | 2.9112 mL | |
| 25 mM | 0.0932 mL | 0.4658 mL | 0.9316 mL | 2.3289 mL | |
| 30 mM | 0.0776 mL | 0.3882 mL | 0.7763 mL | 1.9408 mL | |
| 40 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4556 mL | |
| 50 mM | 0.0466 mL | 0.2329 mL | 0.4658 mL | 1.1645 mL | |
| 60 mM | 0.0388 mL | 0.1941 mL | 0.3882 mL | 0.9704 mL | |
| H2O | 80 mM | 0.0291 mL | 0.1456 mL | 0.2911 mL | 0.7278 mL |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2329 mL | 0.5822 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
ZK756326 dihydrochloride Related Classifications
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