货号 | 4528/10 |
别名 | N-1-[(3-4(-Ethoxyphenyl)-3,4-dihydr |
供应商 | Tocris |
生物活性 | 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 (Cat. No. 4487). |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 605.58 |
分子式 | C32H27F4N5 |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
参考文献 | Verzijlet 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. Storelliet 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. Heiseet al (2005) Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J.Pharmacol.Exp.Ther. 313 1263. PMID: 15761110. |