丙酸氟替卡松, 糖皮质激素受体激动剂

Glucocorticoid Receptor Agonists
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货号 (SKU) 包装规格 是否现货 价格 数量
F409005-1ml
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Compound libraries (12326)

基本描述

英文别名 CCI-187881 | (6α,​11β,​16α,​17α)​-androsta-​1,​4-​diene-​17-​carbothioic acid-6,​9-​difluoro-​11-​hydroxy-​16-​methyl-​3-​oxo-​17-​(1-​oxopropoxy)​-​S-​(fluoromethyl) ester
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Fluticasone propionate
生化机理 丙酸氟替卡松(CCI-187881)是一种合成糖皮质激素,用于治疗非过敏性和过敏性鼻炎。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 激动剂
作用机制 糖皮质激素受体激动剂
产品介绍

Fluticasone propionate 是一种合成的皮质类固醇,是Fluticasone的衍生物,用于治疗哮喘和过敏性鼻炎(花粉症)。A high-affinity, selective glucocorticoid receptor agonist.

Information

Fluticasone propionate Fluticasone Propionate (CCI-187881) is a synthetic glucocorticoid , used to treat non-allergic and allergic rhinitis.
In vitro

Fluticasone propionate (1 pM) inhibits the constitutive and TGF-beta-induced expression of alpha-SMA in human lung myofibroblasts. Fluticasone propionate blocks the TNF-alpha-induced nuclear translocation of the pro-inflammatory transcription factor NF-kappaB in human lung myofibroblasts. Fluticasone propionate inhibits in lung myofibroblasts, at a very early stage of differentiation, the activation of Janus kinase/STAT pathways induced by IL-13 (tyrosine kinase 2, STAT1, STAT3, STAT6, mitogen-activated protein kinase). Fluticasone propionate still displays a potential anti-inflammatory activity even if it only inhibits tyrosine kinase 2 phosphorylation in mildly or fully differentiated myofibroblastic cultures. Fluticasone propionate inhibits constitutive and TGF-beta-induced expression of alpha-smooth muscle actin, the main marker of myofibroblastic differentiation, both in very early and in mild differentiated myofibroblasts. Fluticasone propionate displays an additional powerful anti-inflammatory effect, decreasing nuclear translocation of NF-kappaB independent of the degree of myofibroblastic differentiation. Fluticasone propionate inhibits allergen-induced T-cell proliferation, expression of IL-3, IL-5 and GM-CSF mRNA, and secretion of the corresponding proteins in a concentration-dependent fashion. Fluticasone propionate has the potential markedly to inhibit allergen-induced T-cell production of asthma-relevant cytokines.

In vivo

Fluticasone propionate administrated after induction of a severe heaves exacerbation results in complete resolution of clinical signs, normalization of pulmonary function tests, and significant decrease in bronchoalveolar lavage (BAL) neutrophilia in horse.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥97%

关联靶点(人)

NR3C1 Tclin 糖皮质激素受体(Glucocorticoid receptor) (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)
PGR Tclin 孕酮受体(Progesterone receptor) (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)
NR3C2 Tclin 盐皮质激素受体(Mineralocorticoid receptor) (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 CCC(=O)OC1(C(C)CC2C3CC(F)C4=CC(=O)C=CC4(C)C3(F)C(O)CC12C)C(=O)SCF
分子量 500.57

安全和危险性(GHS)

质量标准

Concentration(Compounding value)
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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. Guozheng Zhao.  (2023)  Multi-Residue Detection of Eight Glucocorticoids by Nano-Au/Fluticasone Propionate Electrochemical Immunosensor.  MOLECULES,  28  (18): (6619).  [PMID:37764395] [10.3390/molecules28186619]
2. Youfang Huang, Yanyun Li, Qing Luo, Xiaojia Huang.  (2021)  One-step preparation of functional groups-rich graphene oxide and carbon nanotubes nanocomposite for efficient magnetic solid phase extraction of glucocorticoids in environmental waters.  CHEMICAL ENGINEERING JOURNAL,  406  (126785).  [10.1016/j.cej.2020.126785]

参考文献

1. Guozheng Zhao.  (2023)  Multi-Residue Detection of Eight Glucocorticoids by Nano-Au/Fluticasone Propionate Electrochemical Immunosensor.  MOLECULES,  28  (18): (6619).  [PMID:37764395] [10.3390/molecules28186619]
2. Youfang Huang, Yanyun Li, Qing Luo, Xiaojia Huang.  (2021)  One-step preparation of functional groups-rich graphene oxide and carbon nanotubes nanocomposite for efficient magnetic solid phase extraction of glucocorticoids in environmental waters.  CHEMICAL ENGINEERING JOURNAL,  406  (126785).  [10.1016/j.cej.2020.126785]

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