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Submit ReviewJ 113863 is a potent chemokine receptor 1 (CCR1) antagonist (IC50 values are 0.9 and 5.8 nM for human and mouse CCR1 receptors respectively). Also displays high selectivity for human but not mouse CCR3 receptors (IC50 values are 0.58 and 460 nM respectively). Improves paw inflammation, joint damage and dramatically reduces cell infiltration into joints in collagen-induced arthritis in mice.
Isomer also available.
分子量 | 655.44 |
公式 | C30H37Cl2IN2O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 202796-41-6 |
PubChem ID | 6918496 |
InChI Key | FOAFBMYSXIGAOX-LQGGPMKRSA-N |
Smiles | ClC1=CC=C(OC(C=CC(Cl)=C3)=C3C2C(N[C@@H]4CC[N@@+](C/C5=C/CCCCCC5)(CC)CC4)=O)C2=C1.ClC6=CC=C(OC(C=CC(Cl)=C8)=C8C7C(N[C@H]9CC[N@+](C/C%10=C/CCCCCC%10)(CC)CC9)=O)C7=C6.[I-].[I-] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 65.54 | 100 | |
ethanol | 32.77 | 50 |
以下数据基于产品分子量 655.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.53 mL | 7.63 mL | 15.26 mL |
5 mM | 0.31 mL | 1.53 mL | 3.05 mL |
10 mM | 0.15 mL | 0.76 mL | 1.53 mL |
50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
参考文献是支持产品生物活性的出版物。
Naya et al (2001) Design, synthesis, and discovery of a novel CCR1 antagonist. J.Med.Chem. 44 1429 PMID: 11311066
Amat et al (2006) Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo. Br.J.Pharmacol. 149 666 PMID: 17016504
If you know of a relevant reference for J 113863, please let us know.
关键词: J 113863, J 113863 supplier, Potent, CCR1, chemokine, receptor, antagonists, CXCR, Receptors, J113863, Rantes, Chemokine, CC, 2595, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 J 113863 的部分引用包括:
Kamata et al (2015) The cholesterol-binding protein NPC2 restrains recruitment of stromal macrophage-lineage cells to early-stage lung tumours. Biomaterials 7 1119 PMID: 26183450
Gibon et al (2012) Effect of a CCR1 receptor antagonist on systemic trafficking of MSCs and polyethylene particle-associated bone loss. ScientificWorldJournal 33 3632 PMID: 22364730
Ansari et al (2022) CCR1 antagonist J-113863 corrects the imbalance of pro- and anti-inflammatory cytokines in a SJL/J mouse model of relapsing-remitting multiple sclerosis. Immunobiology 227 152245 PMID: 35868215
Rowe et al (2014) PGC-1α induces SPP1 to activate macrophages and orchestrate functional angiogenesis in skeletal muscle. Circ Res 115 504 PMID: 25009290
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J113863 was used in a chemotaxis assay using a subset of C57Bl/6 splenic cells. Cells were pretreated with J113863 for 2 hours before being added to the top portion of a transwell assay. CCL6 or media was used and the chemoattractant and cells were given 2 hours to migrate.
As best we can tell, J113863 is entirely insoluble in water containing media. The drug was first dissolved in DMSO, and PBS added to bring to 5% DMSO. As soon as the PBS is added, the drug comes out of solution, however it has proven to still be effective in vitro at concentrations of approximately 1ug/ml and 10ug/ml
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.