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Submit ReviewRS 102895 hydrochloride is a CCR2-selective chemokine receptor antagonist (IC50 values are 0.36 and 17.8 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC50 values of 32 nM and 1.7 μM respectively. Also inhibits α1A, α1D and 5-HT1A receptors.
RS 102895 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 426.86 |
公式 | C21H21F3N2O2.HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 1173022-16-6 |
PubChem ID | 16759153 |
InChI Key | KRRISOFSWVKYBF-UHFFFAOYSA-N |
Smiles | Cl.FC(F)(F)C1=CC=C(CCN2CCC3(CC2)OC(=O)NC2=CC=CC=C32)C=C1 |
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 | 32.01 | 75 |
以下数据基于产品分子量 426.86。 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 |
---|---|---|---|
0.75 mM | 3.12 mL | 15.62 mL | 31.24 mL |
3.75 mM | 0.62 mL | 3.12 mL | 6.25 mL |
7.5 mM | 0.31 mL | 1.56 mL | 3.12 mL |
37.5 mM | 0.06 mL | 0.31 mL | 0.62 mL |
参考文献是支持产品生物活性的出版物。
Clark et al (1983) Synthesis and antihypertensive activity of 4'-substituted spiro[4H-3,1-benzoxazine-4,4'piperidin]-2(1H)-ones. J.Med.Chem. 26 657 PMID: 6842505
Mirzadegan et al (2000) Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists. J.Biol.Chem. 275 25562 PMID: 10770925
If you know of a relevant reference for RS 102895 hydrochloride, please let us know.
关键词: RS 102895 hydrochloride, RS 102895 hydrochloride supplier, CCR2b, chemokine, receptor, antagonists, Chemokine, Receptors, RS102895, hydrochloride, CC, 2089, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RS 102895 hydrochloride 的部分引用包括:
Teng et al (2017) Blocking the CCL2-CCR2 Axis Using CCL2-Neutralizing Antibody Is an Effective Therapy for Hepatocellular Cancer in a Mouse Model. Mol Cancer Ther 16 312 PMID: 27980102
Maxwell et al (2014) Tumor-derived CXCL8 signaling augments stroma-derived CCL2-promoted proliferation and CXCL12-mediated invasion of PTEN-deficient prostate cancer cells. Oncotarget 5 4895 PMID: 24970800
Sennlaub et al (2013) CCR2(+) monocytes infiltrate atrophic lesions in age-related macular disease and mediate photoreceptor degeneration in experimental subretinal inflammation in Cx3cr1 deficient mice. EMBO Mol Med 5 1775 PMID: 24142887
Hung et al (2013) Monocyte chemoattractant protein-1 affects migration of hippocampal neural progenitors following status epilepticus in rats. J Neuroinflammation 10 11 PMID: 23339567
Cerri et al (2016) The Chemokine CCL2 Mediates the Seizure-enhancing Effects of Systemic Inflammation. J Neurosci 36 3777 PMID: 27030762
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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.