白藜芦醇, COX-2 抑制剂;TAS2R14 激动剂;过氧化物酶体增殖激活受体-γ 拮抗剂

IKK Selective Inhibitors | Modulators
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货号 (SKU) 包装规格 是否现货 价格 数量
R408711-1ml
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Compound libraries (12326)

基本描述

英文别名 trans-Resveratrol | (E)-5-(4-hydroxystyryl)benzene-1,3-diol
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Resveratrol (SRT501)
生化机理 白藜芦醇(SRT501,反式白藜芦醇)具有广泛的靶标,包括环氧化酶(即 COX,IC50=1.1 μM)、脂氧化酶(LOX,IC50=2.7 μM)、激酶、sirtuins 和其他蛋白质。它具有抗癌、抗炎、降血糖和其他有益心血管的作用。白藜芦醇能诱导有丝分裂/自噬和依赖自噬的细胞凋亡。
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 COX-2 抑制剂;TAS2R14 激动剂;过氧化物酶体增殖激活受体-γ 拮抗剂
产品介绍

无味,完全溶解于乙醇。 COX−1选择性抑制剂。 白藜芦醇是一种酚类植物抗毒素,发现于葡萄皮和其他植物中。它具有细胞内抗氧化活性激活去乙酰化酶SIRT1。白藜芦醇的抗糖尿病、神经保护和抗脂特性都可能是去乙酰化酶SIRT1激活所致。

Information

Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e.COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and
In vitro

Resveratrol inhibits the activity of Cyclooxygenase and lipooxygenase, PKCs and p56lck, ERK1, JNK1, p38, IKK β, Src, STAT3, Ribonucleotide Reductase, DNA polymerases α and δ, PKD, PKC α, Quinone reductase 2, and Aromatase with IC50 of from 0.035-60 μM. Resveratrol is also an activator of Adenylyl cyclase and AMPK with EC50 of 0.8 μM and 50 μM, respectively. The roles of Resveratrol as inhibitor or activator enable its effects on decreasing cell inflammatory associated behaviors, growth inhibition and induction of apoptosis in cancer cells, reversal of endothelin-1 stimulated cell responses, inhibition of phorbol ester-induced expression of COX-2, inhibition of DNA synthesis in cell, resistance to menadione-induced cell death, and improvement of cell mitochondrial function and glucose/lipid metabolism. Resveratrol is also an activator of sirtuins. Resveratrol lowers the Michaelis constant of SIRT1 for both the acetylated substrate and NAD+, and increases cell survival by stimulating SIRT1-dependent deacetylation of p53. In yeast, Resveratrol mimics calorie restriction by stimulating Sir2, increasing DNA stability and extending lifespan. Resveratrol is effective at protecting isolated rat hearts against ischemia/reperfusion injury via its antioxidant activity, with improved recovery of developed pressure and aortic flow, reduction of malondialdehyde concentrations and reduction of infarct size.

In vivo

Resveratrol improves health and survival of mice on a high-calorie diet. Resveratrol (22.4 mg/kg/day) shifts the physiology of middle-aged mice on a high-calorie diet towards that of mice on a standard diet and significantly increases their survival. Resveratrol produces changes associated with longer lifespan, including increased insulin sensitivity, reduced insulin-like growth factor-1 (IGF-I) levels, increased AMP-activated protein kinase (AMPK) and peroxisome proliferator-activated receptor-γcoactivator 1α(PGC-1α) activity, increased mitochondrial number, and improved motor function. Resveratrol opposed the effects of the high-calorie diet in 144 out of 153 significantly altered pathways. Resveratrol has been shown to inhibit the initiation and growth of tumors in a wide variety of rodent cancer models. Dose of Resveratrol as low as 200 μg/kg daily already shows efficacy in a rat model of colon carcinogenesis. At higher dose of 40 mg/kg, Resveratrol increases the survival of mice with subcutaneous neuroblastomas from 0% to 70%. Resveratrol inhibits vascularization in the corneal micropocket assay in mice at a dose of only 48 μg/kg when administered daily. Resveratrol shows beneficial effects on heart disease. Resveratrol blocks the increase in platelet aggregation induced by a hypercholesterolaemic diet. Resveratrol increase expression of both endothelial and inducible nitric oxide synthase. In stroke-prone, spontaneously hypertensive rats, resveratrol significantly reduces markers of oxidative stress such as glycated albumin in serum, and 8-hydroxyguanos-ine in urine. Providing Resveratrol in drinking water for 15 days (1 mg/kg) is sufficient to improve the recovery in function and coronary flow of isolated hearts. Resveratrol displays anti-inflammatory activity in vivo. Resveratrol significantly reduces both acute and chronic chemically induced oedema, lipopolysaccharide-induced airway inflammation and osteoarthritis, and helps to prevent allograft rejection. Intravenously administered Resveratrol decreases inflammation induced by ischaemia/reperfusion, oxidants generated by hypoxanthine/xanthine oxidase (HX/XO) or platelet-activating factor, but not leukotriene B4 in rats. Resveratrol shows beneficial effects on stroke and brain damage. Resveratrol administered intravenously significantly decreased ischaemic volume and brain water content at the extremely low doses of 100 ng/kg and 1 μg/kg after middle cerebral artery occlusion in rats.
Cell Data

cell lines:

Concentrations:30-300 μM

Incubation Time:2 days

Powder Purity:≥99%

产品属性

IC50 IKK β, IC50: 1 μM

关联靶点(人)

CYP1B1 Tchem 细胞色素 P450 1B1(Cytochrome P450 1B1) (2 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)
CYP3A4 Tclin 细胞色素P450 3A4(Cytochrome P450 3A4) (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)
DPP4 Tclin 二肽基肽酶4(Dipeptidyl peptidase 4) (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)
TRPA1 Tclin 瞬时受体电位阳离子通道亚家族A成员1(Transient receptor potential cation channel subfamily A member 1) (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)
TTR Tclin 转甲状腺素蛋白(Transthyretin) (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)
PTGS1 Tclin 前列腺素 G/H 合酶 1(Prostaglandin G/H synthase 1) (2 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)
PTGS2 Tclin 前列腺素 G/H 合酶 2(Prostaglandin G/H synthase 2) (5 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)
CA12 Tclin 碳酸酐酶12(Carbonic anhydrase 12) (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)
CA14 Tclin 碳酸酐酶14(Carbonic anhydrase 14) (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)
CA9 Tclin 碳酸酐酶9(Carbonic anhydrase 9) (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)
NQO2 Tchem 核糖二氢烟酰胺脱氢酶[醌](Ribosyldihydronicotinamide dehydrogenase [quinone]) (9 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)
PPARG Tclin 过氧化物酶体增殖激活受体γ(Peroxisome proliferator-activated receptor gamma) (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 OC1=CC=C(C=C1)\C=C\C2=CC(=CC(=C2)O)O
分子量 228.24

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 38 mg/mL (197.74 mM);    

安全和危险性(GHS)

质量标准

Concentration(Compounding value) 9.8-10.2(mmol/L)
Appearance(R408711) Colorless Transparent Liquid
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:

溶液计算器