计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，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
2-8°C储存,避光,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
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
AM 103 is a potent and selective FLAP inhibitor, with an IC 50 value of 4.2 nM.
In Vitro
AM 103 has an IC 50 value of 349 nM in the human blood LTB4 inhibition assay. AM 103 has an excellent CYP profile against the 5 most common CYP isoforms with IC 50 values greater than 30 μM for CYP2D6 and >50 μM for CYPs 3A4, 2C9 2C19, and 1A2. AM103 is a novel, potent, and selective FLAP inhibitor with IC 50 values of 350, 113, and 117 nM against human, rat, and mouse whole-blood ionophore-stimulated LTB4 production, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AM 103 has high bioavailability (64%), low clearance (2.9 mL/min/kg), low volume of distribution (0.41 L/kg), and a long i.v. half-life (5.2 h) in dogs. AM 103 (10 mg/kg q.i.d.) inhibits the increase in CysLTs and EPO by approximately 60%, and IL-5 levels are reduced to the concentrations obtained following saline treatment alone in mice . AM103 (1 mg/kg, p.o.) displays >50% inhibition for up to 6 h with a calculated EC 50 of appr 60 nM, in a rat ex vivo whole-blood calcium ionophore-induced LTB4 assay. AM 103 inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED 50 values of 0.8 and 1 mg/kg, respectively, when rat lung is challenged in vivo with calcium ionophore. In this model, the EC 50 derived from plasma AM103 is appr 330 nM for inhibition of both LTB4 and CysLT. In a model of chronic lung inflammation using ovalbumin-primed and challenged BALB/c mice, AM103 reduces the concentrations of eosinophil peroxidase, CysLTs, and interleukin-5 in the bronchoalveolar lavage fluid. Finally, AM 103 increases survival time in mice exposed to a lethal intravenous injection of platelet-activating factor. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 4.2 nM (FLAP)
规格
规格或纯度
≥99%
英文名称
AM103
生化机理
AM 103 是一种强效的选择性 FLAP 抑制剂，其 IC 50 值为 4.2 nM。
储存条件
2-8°C储存,避光,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
INCHI
1S/C36H39N3O4S.Na/c1-35(2,3)44-33-29-19-28(43-23-27-9-7-8-18-37-27)15-16-30(29)39(31(33)20-36(4,5)34(40)41)22-24-10-12-25(13-11-24)26-14-17-32(42-6)38-21-26;/h7-19,21H,20,22-23H2,1-6H3,(H,40,41);
InChi Key
VANSVYMYESBUFV-UHFFFAOYSA-N
Smiles
CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=CC=CC=N3)CC4=CC=C(C=C4)C5=CN=C(C=C5)OC)CC(C)(C)C(=O)O.[Na]
PubChem CID
MeSH Entry Terms
3-(3-tert-butylsulfanyl-1-(4-(6-methoxypyridin-3-yl)benzyl)-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropionic acid;AM 103;AM-103;AM103
分子量
631.76
技术文档
高级数据
三维结构
交互式化学结构模型
化学和物理性质
溶解性
DMSO : 200 mg/mL (316.58 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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