计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，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
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 130 篇同行评审文献引用。
概述
芹菜素属于多酚类黄酮类化合物，以植物黄色素的形式存在于多种植物中，吡啶水溶液呈黄色针晶，无嗅无味。几乎不溶于水，部分溶于热酒精，溶于稀KOH溶液。 黄酮类化合物(flavonoid),能捕获细胞周期的G2/M期，抑制细胞扩增。抑制生长，诱发凋亡，具有抑制致癌物质的致癌活性。
应用
LC-ESI-MS/MS 可作为内标物，用于测定大鼠血液和尿液中的飞燕草苷及其代谢产物。
Information
Apigenin (NSC 83244, LY 080400) is a potentP450inhibitor for CYP2C9 withKiof 2 μM.
In vitro
Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). Apigenin also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. Apigenin exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. Apigenin has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. Apigenin suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. Apigenin has been reported to inhibit protein kinase C activity, mitogen-activated protein kinase (MAPK), transformation of C3HI mouse embryonic fibroblasts and downstream oncogenes in v-Ha-ras-transformed NIH3T3 cells. Apigenin blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. Apigenin has further been shown to down-regulate the expression of the Na+/Ca2+-exchanger, a protein important for calcium extrusion in neonatal rat cardiac myocytes. Apigenin induces a reversible G2/M and G0/G1 arrest by inhibiting p34 (cdc2) kinase activity, accompanied by increased p53 protein stability in epidermal cells and fibroblasts. Apigenin is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. Apigenin inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. Apigenin inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. Apigenin also inhibits proliferating of human keratinocytes.
In vivo
Apigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. Apigenin inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. Apigenin is shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice (64) and also suppresses prostate and breast cancer cell growth through estrogen receptor β1. Apigenin suppresses the levels of IGF-I in prostate tumor xenografts and increases levels of IGFBP-3, a binding protein that sequesters IGF-I in vascular circulation. Apigenin (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice.
Cell Data
cell lines：
Concentrations：0, 1, 5, 10, 20, 30, 40, and 50 μg/ml
Incubation Time：24 h
Powder Purity:≥97%
规格
英文别名
NSC 83244 | 4H-1-Benzopyran-4-one, 5,7-dihydroxy-2-(4-hydroxyphenyl)-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Apigenin (LY 080400)
生化机理
芹菜素（NSC 83244，LY 080400）是一种强效的 P450 CYP2C9 抑制剂，Ki为 2 μM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激活剂
作用机制
CFTR 激活剂
名称和识别符
EC号
208-292-3
分子类型
小分子
Isomeric SMILES
C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O
分子量
270.24
Beilstein号
262620
Reaxy-Rn
262620
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=262620&ln=
技术文档
高级数据
关联靶点（人）
CYP1A2
Tchem
细胞色素 P450 1A2(Cytochrome P450 1A2)
(3 活性数据)
CYP1B1
Tchem
细胞色素 P450 1B1(Cytochrome P450 1B1)
(3 活性数据)
CFTR
Tclin
囊性纤维化跨膜传导调节器(Cystic fibrosis transmembrane conductance regulator)
(1 活性数据)
DPP4
Tclin
二肽基肽酶4(Dipeptidyl peptidase 4)
(1 活性数据)
HSD17B1
Tchem
雌二醇 17-β-脱氢酶 1(Estradiol 17-beta-dehydrogenase 1)
(1 活性数据)
PSMB5
Tclin
蛋白酶体亚基β5型(Proteasome subunit beta type-5)
(1 活性数据)
TTR
Tclin
转甲状腺素蛋白(Transthyretin)
(2 活性数据)
CYP19A1
Tclin
芳香化酶(Aromatase)
(2 活性数据)
CYP1A1
Tchem
细胞色素 P450 1A1(Cytochrome P450 1A1)
(2 活性数据)
XDH
Tclin
黄嘌呤脱氢酶/氧化酶(Xanthine dehydrogenase/oxidase)
(2 活性数据)
ACHE
Tclin
乙酰胆碱酯酶(Acetylcholinesterase)
(1 活性数据)
MAOA
Tclin
胺氧化酶[含黄素]A(Amine oxidase [flavin-containing] A)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro
熔点
345-350°C
安全和危险性（GHS）
信号词
警告
危险声明
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
WGK Germany
3
RTECS
LK9276000
Merck Index
730
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:
技术文档和文章
此产品的引用文献
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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