计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
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文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
NBI-74330 is a potent antagonist for CXCR3 , and exhibits potent inhibition of ( 125 I)CXCL10 and ( 125 I)CXCL11 specific binding with K i of 1.5 and 3.2 nM, respectively.
In Vitro
BI-74330 demonstrates potent inhibition of [ 125 I]CXCL11 specific binding to membranes prepared from transfected CHO cells expressing CXCR3 (CXCR3-CHO) (K i =3.6 nM). NBI-74330 is 12- and 3.5-fold more potent than CXCL9 (K i =45.2 nM) and CXCL10 (K i =12.5 nM), respectively, at inhibiting [ 125 I]CXCL11 binding to CXCR3-CHO cell membranes. NBI-74330 inhibits calcium mobilization in response to CXCL11 and CXCL10 with an IC 50 value of 7 nM for both ligands used at their EC 80 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 [ 35 S]GTPγS binding in membranes of cells endogenously expressing CXCR3 (H9 cells, IC 50 value 5.5 nM). BI-74330 inhibits CXCL11-induced chemotaxis in these cells with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:[ 125 I]CXCL10-CXCR3 1.5 nM (Ki, in CXCR3-CHO cell membranes) [ 125 I]CXCL11-CXCR3 3.2 nM (Ki, in CXCR3-CHO cell membranes)
规格
规格或纯度
10mM in DMSO
英文名称
NBI-74330
生化机理
NBI-74330 是一种强效的 CXCR3 拮抗剂，可有效抑制 ( 125 I)CXCL10 和 ( 125 I)CXCL11 的特异性结合，其 K i 分别为 1.5 和 3.2 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCOC1=CC=C(C=C1)N2C(=O)C3=C(N=CC=C3)N=C2C(C)N(CC4=CN=CC=C4)C(=O)CC5=CC(=C(C=C5)F)C(F)(F)F
MeSH Entry Terms
N-1R-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido(2,3-d)pyrimidin-2-yl)-ethyl-N-pyridin-3-ylmethyl-2-(4-fluoro-3-trifluoromethylphenyl)acetamide;NBI-74330
分子量
605.58
Reaxy-Rn
11147943
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11147943&ln=
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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