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ZK756326 2HCl CCR agonist

Cat.No.S8324

ZK756326 is a full agonist of CCR8(Chemokine receptor 8) with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.
ZK756326 2HCl CCR agonist Chemical Structure

Chemical Structure

Molecular Weight: 429.38

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Quality Control

Batch: S832401 Water]78 mg/mL]false]DMSO]39 mg/mL]false]Ethanol]4 mg/mL]false Purity: 99.01%
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99.01

Solubility

In vitro
Batch:

Water : 78 mg/mL

DMSO : 39 mg/mL (90.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 429.38 Formula

C21H28N2O3.2HCl

Storage (From the date of receipt)
CAS No. 874911-96-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCN1CCOCCO)CC2=CC(=CC=C2)OC3=CC=CC=C3

Mechanism of Action

Targets/IC50/Ki
CCR8
(in U87 cell line)
1.8 μM
In vitro
ZK 756326 stimulated extracellular acidification in cells expressing human CCR8. The ability of ZK 756326 to induce a response was receptor-specific and mediated through Gαi, because it could be blocked by treatment with pertussis toxin. Like CCL1, ZK 756326 inhibited human immunodeficiency virus (HIV) fusion of cells expressing CD4 and CCR8. But unlike mCCL1, ZK 756326 bound to and activated a form of mCCR8 that was mutated to eliminate O-linked sulfation at tyrosines 14 and 15. Therefore, ZK 756326 is most probably not binding in the same manner as CCL1 but can activate the switch mechanism involved in transducing signaling events.
References

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