688352-84-3
688352-84-3 structure
- Name: R243
- Chemical Name: R243
- CAS Number: 688352-84-3
- Molecular Formula: C21H27NO4
- Molecular Weight: 357.45
- Catalog: Signaling Pathways GPCR/G Protein CCR
- Create Date: 2020-01-17 22:23:36
- Modify Date: 2024-01-21 17:02:28
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R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM; attenuated secretion of TNF-α, IL-6, and most strikingly IL-10 from WT PMφ (peritoneal macrophages), but not BMMφ (bone marrow-derived macrophages); shows suppressed c-JNK activity and NF-κB signaling after LPS treatment, suppresses LPS-induced cytokine secretion; attenuates peritoneal adhesions in vivo in CCR8-/- mice, also prevents hapten-induced colitis.
| Name | R243 |
|---|
| Description | R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM; attenuated secretion of TNF-α, IL-6, and most strikingly IL-10 from WT PMφ (peritoneal macrophages), but not BMMφ (bone marrow-derived macrophages); shows suppressed c-JNK activity and NF-κB signaling after LPS treatment, suppresses LPS-induced cytokine secretion; attenuates peritoneal adhesions in vivo in CCR8-/- mice, also prevents hapten-induced colitis. |
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| References | References 1. Oshio T, et al. PLoS One. 2014 Apr 8;9(4):e94445. 2. Berenguer J, et al. J Extracell Vesicles. 2018 Mar 13;7(1):1446660. View Related Products by Target Chemokine Receptor (CCR and CXCR) |
| Molecular Formula | C21H27NO4 |
|---|---|
| Molecular Weight | 357.45 |
| Storage condition | -20°C |