1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. ZK756326 dihydrochloride

ZK756326 dihydrochloride 

Cat. No.: HY-101038A Purity: 98.28%
Handling Instructions

ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

For research use only. We do not sell to patients.

ZK756326 dihydrochloride Chemical Structure

ZK756326 dihydrochloride Chemical Structure

CAS No. : 1780259-94-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 114 In-stock
Estimated Time of Arrival: December 31
25 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
100 mg USD 588 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

IC50 & Target[1]

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)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

429.38

Formula

C₂₁H₃₀Cl₂N₂O₃

CAS No.

1780259-94-0

SMILES

OCCOCCN1CCN(CC2=CC=CC(OC3=CC=CC=C3)=C2)CC1.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (116.45 mM; Need ultrasonic)

DMSO : 27.5 mg/mL (64.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3289 mL 11.6447 mL 23.2894 mL
5 mM 0.4658 mL 2.3289 mL 4.6579 mL
10 mM 0.2329 mL 1.1645 mL 2.3289 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

ZK756326ZK 756326ZK-756326CCRCC chemokine receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ZK756326 dihydrochloride
Cat. No.:
HY-101038A
Quantity:
MCE Japan Authorized Agent: