J 113863

Pricing Availability   Qty
说明: Potent CCR1 chemokine receptor antagonist
化学名: 1,4-cis-1-(1-Cycloocten-1-ylmethyl)-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethylpiperidinium iodide
纯度: ≥98% (HPLC)
说明书
引用文献 (4)
评论 (1)
文献 (1)

生物活性 for J 113863

J 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.

技术数据 for J 113863

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.

溶解性数据 for J 113863

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 65.54 100
ethanol 32.77 50

制备储备液 for J 113863

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for J 113863

分析证书/产品说明书
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参考文献 for J 113863

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.

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查看全部 Chemokine CC Receptor Antagonists

关键词: J 113863, J 113863 supplier, Potent, CCR1, chemokine, receptor, antagonists, CXCR, Receptors, J113863, Rantes, Chemokine, CC, 2595, Tocris Bioscience

4 篇 J 113863 的引用文献

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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J 113863 的评论

平均评分: 5 (Based on 1 Review.)

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Effective in blocking mouse CCL6 chemotaxis in vitro.
By Anonymous on 12/12/2017
分析类型: In Vitro
种属: Mouse
细胞系/组织: Splenic Cells

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

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该领域的文献

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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。


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