货号	规格	价格	上海	北京	珠海	重庆	武汉
S86774-5mg	≥98%	￥1230.00 S86774-5mg ￥1230.00 3-5天	0 货期：3-5天	-	-	-	-
S86774-10mg	≥98%	￥2060.00 S86774-10mg ￥2060.00 3-5天	0 货期：3-5天	-	-	-	-
S86774-50mg	≥98%	￥5760.00 S86774-50mg ￥5760.00 3-5天	0 货期：3-5天	-	-	-	-
S86774-100mg	≥98%	￥9220.00 S86774-100mg ￥9220.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.

靶点：

[125I]CXCL10-CXCR3:1.5 nM (Ki, in CXCR3-CHO cell membranes);[125I]CXCL11-CXCR3:3.2 nM (Ki, in CXCR3-CHO cell membranes)

体外研究：

BI-74330 demonstrates potent inhibition of [125I]CXCL11 specific binding to membranes prepared from transfected CHO cells expressing CXCR3 (CXCR3-CHO) (Ki=3.6 nM). NBI-74330 is 12- and 3.5-fold more potent than CXCL9 (Ki=45.2 nM) and CXCL10 (Ki=12.5 nM), respectively, at inhibiting [125I]CXCL11 binding to CXCR3-CHO cell membranes. NBI-74330 inhibits calcium mobilization in response to CXCL11 and CXCL10 with an IC50 value of 7 nM for both ligands used at their EC80 concentrations (1 nM for CXCL11 and 30 nM for CXCL10). NBI-74330 specifically inhibits CXCR3-mediated calcium mobilization. NBI-74330 also dose-dependently inhibits CXCL11-induced [35S]GTPγS binding in membranes of cells endogenously expressing CXCR3 (H9 cells, IC50 value 5.5 nM). BI-74330 inhibits CXCL11-induced chemotaxis in these cells with an IC50 of 3.9 nM. NBI-74330 (30-300 nm, 1-10 μM) produces concentration-dependent, parallel rightward shifts of the CXCL11 E/[A] curve with no significant change in the E/[A] curve maximal response.

体内研究：

NBI-74330 (100 mg/kg) results in the formation of an N-oxide metabolite, also an antagonist of CXCR3, in mice. Mice treated with 100 mg/kg NBI-74330 (in 1% Na Doc in 0.5% 400Cp Methylcellulose) result in serum concentrations of approximately 1 μM. This concentration is sufficient to fully block the CXCR3 receptor in vivo

参考文献：

1. Heise CE, et al. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J Pharmacol Exp Ther. 2005 Jun;313(3):1263-71. 2. Jopling LA, et al. Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay. Br J Pharmacol. 2007 Dec;152(8):1260-71. 3. van Wanrooij EJ, et al. CXCR3 antagonist NBI-74330 attenuates atherosclerotic plaque formation in LDL receptor-deficient mice. Arterioscler Thromb Vasc Biol. 2008 Feb;28(2):251-7.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.651 ml	8.257 ml	16.513 ml
5 mM	0.33 ml	1.651 ml	3.303 ml
10 mM	0.165 ml	0.826 ml	1.651 ml
50 mM	0.033 ml	0.165 ml	0.33 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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