萘丁美酮, 环氧化酶-2 抑制剂

COX Inhibitors
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
N408414-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 BRL-14777 | 2-Butanone, 4-(6-methoxy-2-naphthalenyl)-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Nabumetone
生化机理 萘丁美酮(BRL-14777)是一种非甾体抗炎药,其活性代谢物可抑制 COX。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 环氧化酶-2 抑制剂
产品介绍

Nabumetone 是一种可口服的非酸类抗炎剂,为有效的、选择性的 COX-2 抑制剂,同时是活性代谢物 6MNA 的前体物质。

Information

Nabumetone Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX .
In vitro

Nabumetone is a nonsteroidal anti-inflammatory prodrug. Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially COX-2.

In vivo

Nabumetone displays acute anti-inflammatory activity in the carrageenan-induced oedema model in rats and the ultraviolet-induced erythema model in guinea-pigs. Its activity in these tests is greater than that of aspirin but less than that of naproxen and indomethacin. In the cotton pellet-induced granuloma model in the rat, Nabumetone is active and produces no signs of toxicity at doses much greater than the lowest effective dose, unlike aspirin, naproxen or indomethacin. Nabumetone is also active in the adjuvant-induced arthritis test in rats. In contrast to aspirin, indomethacin and naproxen, Nabumetone is well tolerated by the stomach of fasted rats at doses in excess of those with anti-inflammatory activity.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 2.943
hba_count 2
Rotatable Bond 4

关联靶点(人)

CYP1A2 Tchem 细胞色素 P450 1A2(Cytochrome P450 1A2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MAOA Tclin 胺氧化酶[含黄素]A(Amine oxidase [flavin-containing] A) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES COC1=CC=C2C=C(CCC(C)=O)C=CC2=C1
分子量 228.29
Reaxy-Rn 2103472
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2103472&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 46
DMSO(mM) Max Solubility 201.5
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 2103472
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2103472&ln=

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

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:

此产品的引用文献

1. Lian Xu, Yan Xiao, Kun Yu, Hongshuo Pan, Jiayi Xu, Yiyun Guan, Mengke Wang, Xiangyu Xu, Hao Wang.  (2025)  Machine Learning-Assisted Chemical Tongues Based on Dual-channel Inclusion Complexes for Rapid Identification of Nonsteroidal Anti-inflammatory Drugs in Food.  ACS Sensors,  [PMID:39992799] [10.1021/acssensors.4c02806]

参考文献

1. Lian Xu, Yan Xiao, Kun Yu, Hongshuo Pan, Jiayi Xu, Yiyun Guan, Mengke Wang, Xiangyu Xu, Hao Wang.  (2025)  Machine Learning-Assisted Chemical Tongues Based on Dual-channel Inclusion Complexes for Rapid Identification of Nonsteroidal Anti-inflammatory Drugs in Food.  ACS Sensors,  [PMID:39992799] [10.1021/acssensors.4c02806]

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