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Submit Review(±)-NBI 74330 is a potent and selective CXCR3 antagonist; potently inhibits 125I-CXCL10 binding to CXCR3 (pKi = 8.13). Inhibits calcium mobilization in response to CXCL11 and CXCL10 in RBL cells. Exhibits no significant effect on chemotaxis induced by CXCR4 or CCR7. Displays a five-fold greater affinity for CXCR3 than (±)-AMG 487.
This product is racemic.
(±)-NBI 74330 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 | 605.58 |
公式 | C32H27F4N5O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 473722-68-8 |
PubChem ID | 10167713 |
InChI Key | XMRGQUDUVGRCBS-UHFFFAOYSA-N |
Smiles | CCOC(C=C3)=CC=C3N2C(C1=CC=CN=C1N=C2C(N(CC4=CC=CN=C4)C(CC5=CC(C(F)(F)F)=C(F)C=C5)=O)C)=O |
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 | 30.28 | 50 |
以下数据基于产品分子量 605.58。 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 |
---|---|---|---|
0.5 mM | 3.3 mL | 16.51 mL | 33.03 mL |
2.5 mM | 0.66 mL | 3.3 mL | 6.61 mL |
5 mM | 0.33 mL | 1.65 mL | 3.3 mL |
25 mM | 0.07 mL | 0.33 mL | 0.66 mL |
参考文献是支持产品生物活性的出版物。
Storelli et al (2007) Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists. Arch.Pharm. 340 281 PMID: 17562560
Verzijl et al (2008) Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. J.Pharmacol.Exp.Ther. 325 544 PMID: 18270317
Heise et al (2005) Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J.Pharmacol.Exp.Ther. 313 1263 PMID: 15761110
If you know of a relevant reference for (±)-NBI 74330, please let us know.
关键词: (±)-NBI 74330, (±)-NBI 74330 supplier, VUF10472, (±)-NBI74330, potent, selective, CXCR3, antagonists, chemokines, (±)-NBI_74330, Chemokine, CXC, Receptors, 4528, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (±)-NBI 74330 的部分引用包括:
Piotrowska et al (2018) Pharmacological blockade of CXCR3 by (±)-NBI-74330 reduces neuropathic pain and enhances opioid effectiveness - Evidence from in vivo and in vitro studies. Biochim.Biophys.Acta 1864 3418 PMID: 30076959
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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!
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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.