R243 |
Catalog No.GC62724
One-Click Copy Product Info
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R243 is a CCR8 receptor inhibitor that suppresses the signaling pathways triggered by CCL1, the endogenous ligand of CCR8.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 688352-84-3
Sample solution is provided at 25 µL, 10mM.
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R243 is a CCR8 receptor inhibitor that suppresses the signaling pathways triggered by CCL1, the endogenous ligand of CCR8[1-2]. R243 is primarily utilized in research related to immune and inflammatory diseases[3].
In vitro, treatment of mouse RAW264.7 macrophages and bone marrow-derived macrophages (BMDMs) with R243 (10µM) for 24 hours significantly inhibited CCL1-driven chemotactic migration in a CCL1-induced (10ng/mL) Transwell migration assay, although the inhibitory effect on the migration of human THP-1 monocytes was not significant [4]. When mouse peritoneal macrophages (PMφ) stimulated with LPS (100ng/mL) were treated with R243 (0–10µM) for 24 hours, R243 significantly suppressed the secretion of TNF-α, IL-6, and IL-10, and reduced the phosphorylation levels of the JNK and NF-κB signaling pathways[5].
In vivo, a peritoneal fibrosis mouse model, R243 (1.0mg/kg; administered via intraperitoneal injection three times a week for 28 days) significantly alleviated chlorhexidine gluconate-induced peritoneal inflammation and fibrosis by functionally inhibiting the CCR8 receptor. This was evidenced by reduced peritoneal thickness, decreased collagen deposition, and diminished macrophage infiltration[6]. In a thermal hyperalgesia test model, R243 (0.3–1mg/kg; administered via intraperitoneal injection 30 minutes prior to CCL1) dose-dependently inhibited CCL1 (10µg/kg)-induced systemic thermal analgesia[7].
References:
[1] Berenguer J, Lagerweij T, Zhao XW, et al. Glycosylated extracellular vesicles released by glioblastoma cells are decorated by CCL18 allowing for cellular uptake via chemokine receptor CCR8. J Extracell Vesicles. 2018 Mar 13;7(1):1446660.
[2] García-Domínguez M, González-Rodríguez S, Hidalgo A, et al. Kappa-opioid receptor-mediated thermal analgesia evoked by the intrathecal administration of the chemokine CCL1 in mice. Fundam Clin Pharmacol. 2021 Dec;35(6):1109-1118.
[3] Ding H, Xu X, Zhu Y, et al. Inhibition of Alkbh5 Attenuates Lipopolysaccharide-Induced Lung Injury by Promoting Ccl1 m6A and Treg Recruitment. Cell Prolif. 2025 Sep;58(9):e70032.
[4] Geervliet E, Arora S, Donohue D, et al. Design, molecular characterization and therapeutic investigation of a novel CCR8 peptide antagonist that attenuates acute liver injury by inhibiting infiltration and activation of macrophages. Acta Pharm Sin B. 2025 Apr;15(4):2114-2133.
[5] Oshio T, Kawashima R, Kawamura YI, et al. Chemokine receptor CCR8 is required for lipopolysaccharide-triggered cytokine production in mouse peritoneal macrophages. PLoS One. 2014 Apr 8;9(4):e94445.
[6] Lee Y, Lee J, Park M, et al. Inflammatory chemokine (C-C motif) ligand 8 inhibition ameliorates peritoneal fibrosis. FASEB J. 2023 Jan;37(1):e22632.
[7] García-Domínguez M, Aguirre A, Lastra A, et al. The Systemic Administration of the Chemokine CCL1 Evokes Thermal Analgesia in Mice Through the Activation of the Endocannabinoid System. Cell Mol Neurobiol. 2019 Nov;39(8):1115-1124.
| Cell experiment [1]: | |
Cell lines | RAW264.7 macrophages (mouse leukemic monocyte/macrophage cell line), THP-1 monocytes (human monocytic cell line), and Bone Marrow-Derived Macrophages (BMDMs) from C57BL/6 mice |
Preparation Method | Cells were maintained in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS), 2mM L-glutamine, and 1% penicillin/streptomycin at 37°C, 5% CO₂. For transwell migration assays, cells were activated with R243 (10μM), LPS (100ng/mL) and IFN-γ (10ng/mL) and seeded in transwell inserts. CCL1(10ng/mL) was added in transwell ousters. For gene expression analysis, RAW264.7 macrophages were activated with R243 (10μM), CCL1(10ng/mL), LPS (100ng/mL) and IFN-γ (10ng/mL). |
Reaction Conditions | 10μM; 24h |
Applications | R243 significantly inhibited CCL1-driven chemotaxis of mouse RAW264.7 macrophages and BMDMs, but not human THP-1 monocytes, in Transwell migration assays. R243 also significantly suppressed the gene expression of pro-inflammatory markers (iNOS and IL-6) and CCR8 in LPS/IFN-γ-activated RAW264.7 macrophages. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Peritoneal fibrosis (PF) was induced in mice via daily intraperitoneal injection of 0.2mL chlorhexidine gluconate (CG) solution (composed of 0.1% CG and 15% ethanol) for 4 weeks. Mice were treated with R243 (1.0mg/kg) via intraperitoneal injection three times a week, starting from day 0 and continuing until day 28. On day 28, mice were sacrificed, and peritoneal tissues were harvested for analysis. |
Dosage form | 1.0mg/kg; i.p.; Three times per week for 4 weeks. |
Applications | R243 treatment significantly ameliorated CG-induced peritoneal fibrosis, as evidenced by reduced peritoneal thickening, decreased collagen deposition, and attenuated peritoneal inflammation. |
References: | |
| Cas No. | 688352-84-3 | SDF | |
| Formula | C21H27NO4 | M.Wt | 357.44 |
| Solubility | DMSO : 125 mg/mL (349.71 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7977 mL | 13.9884 mL | 27.9767 mL |
| 5 mM | 559.5 μL | 2.7977 mL | 5.5953 mL |
| 10 mM | 279.8 μL | 1.3988 mL | 2.7977 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)