1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. R243

R243 

Cat. No.: HY-122219
Handling Instructions

R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects.

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

R243 Chemical Structure

R243 Chemical Structure

CAS No. : 688352-84-3

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Description

R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects[1][2].

IC50 & Target[1]

CCR8

 

In Vitro

R243 has CCR8-antagonistic effects on CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation[1].
R243 attenuates secretion of TNF-α, IL-6, and most strikingly IL-10 from wild-type peritoneal macrophages (WT PMφ)[1].
R243-treated WT PMφ shows suppressed c-jun N-terminal kinase activity and NF-κB signaling after lipopolysaccharide (LPS) treatment when compared with WT PMφ[1].

In Vivo

R243 (0.1-1 mg/kg; intraperitoneal injection; once; male Swiss mice) treatment inhibits the analgesic effect evoked by CCL1 in a dose-dependent manner[2].

Animal Model: Male Swiss mice (7-9 weeks old) injected with CCL1[2]
Dosage: 0.1 mg/kg, 0.3mg/kg, 1 mg/kg
Administration: Intraperitoneal injection; once
Result: The analgesic effect evoked by CCL1 (10 μg/kg; 1 h; s.c.) was dose-dependently inhibited.
Molecular Weight

357.44

Formula

C₂₁H₂₇NO₄

CAS No.

688352-84-3

SMILES

[[email protected]@H]12CC(C[[email protected]](C3)C1)(C[[email protected]@H]3C2)OCCN4CC(C=C(OCO5)C5=C6)=C6OC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

R243R 243R-243CCRCC chemokine receptorCCL1CCR8antinociceptiveanti-inflammatorycolitisTNF-αIL-6IL-10chemotaxisInhibitorinhibitorinhibit

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R243
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HY-122219
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