非洛地平, CFTR 激活剂

Calcium Channel Inhibitors

2篇引用文献

Moligand™

10mM in DMSO

CAS编号: 72509-76-3(DMSO)
分子式: C₁₈H₁₉Cl₂NO₄
分子量: 384.25

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
F408159-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	CGH-869 \| 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid-3-ethyl 5-methyl ester
规格或纯度	Moligand™, 10mM in DMSO
英文名称	Felodipine
生化机理	选择性L型Ca 2+通道阻滞剂。在N，R，P / Q和T型通道上可选。显示高的血管选择性，并显示体内抗高血压作用。口服具有活性
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	激活剂
作用机制	CFTR 激活剂
产品介绍	L-型钙通道阻断剂 Information Felodipine Felodipine (CGH-869) is a selective L-type Ca 2+ channel blocker with IC50 of 0.15 nM. In vitro Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM). Felodipine significantly induces the transcription and secretion of IL-6 and IL-8 with ED50 values of 5.8 nM and 5.3 nM in primary human VSMC and lung fibroblasts, respectively, while propranolol or furosemide fails to affect the expression of the two IL genes. Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM. Felodipine at low concentration of 0.1 μM is sufficient to increases NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in rat endothelial cells. Felodipine (10 μM) reduces nuclear translocation of p42/44 mitogen-activated protein kinase and Elk-1 activation stimulated by PDGF-BB, leading to the inhibition of human SMC proliferation. Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM. In vivo Oral administration of Felodipine significantly reduces the average blood pressure (BP) in rats with 5/6 renal ablation, but causes additional impairment of the already impaired renal autoregulation. Administration of Felodipine significantly reduces systolic blood pressure (SBP), serum insulin, intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by blocking NF-κB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response. Cell Data cell lines：MT-4 Concentrations： Incubation Time： Powder Purity:≥99%

产品属性

ALogP	3.549
hba_count	4
HBD Count	1
Rotatable Bond	6

关联靶点（人）

CFTR Tclin 囊性纤维化跨膜传导调节器(Cystic fibrosis transmembrane conductance regulator) (1 活性数据)

点击查看靶蛋白信息： CFTR

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

Canonical SMILES	CCOC(=O)C1=C(C)NC(=C(C1C2=CC=CC(=C2Cl)Cl)C(=O)OC)C
分子量	384.25
Reaxy-Rn	4331472
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4331472&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility	77
DMSO(mM) Max Solubility	200.39
Water(mg / mL) Max Solubility	<1

安全和危险性（GHS）

Reaxy-Rn	4331472
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4331472&ln=

SDS英文版

技术规格说明书

Concentration	9-11（mmol/L）
Proton NMR spectrum	Conforms to Structure

技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

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此产品的引用文献

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1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo. (2024) Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection. JOURNAL OF FOOD COMPOSITION AND ANALYSIS, 126 (17): (105825). [PMID:17580304] [10.1016/j.jfca.2023.105825]
2. Yin Xuezhi, Pan Hao, Liu Hongfei. (2019) A Novel Micron-Size Particulate Formulation of Felodipine with Improved Release and Enhanced Oral Bioavailability Fabricated by Coaxial Electrospray. AAPS PHARMSCITECH, 20 (7): (1-8). [PMID:31407104] [10.1208/s12249-019-1495-8]

参考文献

1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo. (2024) Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection. JOURNAL OF FOOD COMPOSITION AND ANALYSIS, 126 (17): (105825). [PMID:17580304] [10.1016/j.jfca.2023.105825]
2. Yin Xuezhi, Pan Hao, Liu Hongfei. (2019) A Novel Micron-Size Particulate Formulation of Felodipine with Improved Release and Enhanced Oral Bioavailability Fabricated by Coaxial Electrospray. AAPS PHARMSCITECH, 20 (7): (1-8). [PMID:31407104] [10.1208/s12249-019-1495-8]