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
概述
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%
规格
英文别名
CGH-869
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
620-472-7
分子类型
小分子
Isomeric SMILES
CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
关联CAS
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=
高级数据
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)
化学和物理性质
熔点
142.0°C-146.0°C
安全和危险性（GHS）
信号词
警告
危险声明
H373: 长期或反复接触可能对器官造成伤害
H302: 吞食有害
H410: 对水生生物毒性极大并具有长期持续影响
H361: 怀疑破坏生育力或未出生的孩子
预防措施声明
P273: 避免释放到环境中。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P405: 密闭存放
P501: 将内容物/容器送到批准的废物处理厂处理
P264: 处理后要彻底洗手。
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P391: 收集溢出物
P330: 漱口
P203: 使用前，获取、阅读并遵守所有安全说明。
P301+P317: 如果被吞咽：请寻求医疗帮助。
P318: 如果暴露或担心，请就医。
P319: 如果你感到不适，请寻求医疗帮助。
WGK Germany
3
RTECS
US7968700
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
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
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