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经验公式(希尔记法):
C20H24N2O6
化学文摘社编号:
分子量:
388.41
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
264-407-7
MDL number:
InChI
1S/C20H24N2O6/c1-11(2)10-28-20(24)17-13(4)21-12(3)16(19(23)27-5)18(17)14-8-6-7-9-15(14)22(25)26/h6-9,11,18,21H,10H2,1-5H3
InChI key
VKQFCGNPDRICFG-UHFFFAOYSA-N
SMILES string
COC(=O)C1=C(C)NC(C)=C(C1c2ccccc2[N+]([O-])=O)C(=O)OCC(C)C
assay
≥98% (HPLC)
form
powder
color
yellow
solubility
DMSO: >10 mg/mL
originator
Bayer
storage temp.
room temp
Quality Level
Gene Information
human ... CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779)
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Application
Nisoldipine has been used:
- as a hit-antagonist to study its effects on oxytocin (OT)-induced myometrial Ca2+-mobilization and its potency to dampen uterine myometrial contractions
- as a calcium channel blocker to study its effects on cell viability in a human hepatic cancer HepG2 and rat renal epithelial NRK52E cell line
- as a component of the external IK1 recording solution to study the action potential in human pluripotent stem cell−derived cardiomyocytes (hiPS-CMs)
Biochem/physiol Actions
L-type (CaV1.2) calcium channel blocker; dihydropyridine-type calcium channel blocker with selectivity for smooth muscle (CaV1.2b) over cardiac muscle (CaV1.2a). Arterial vasodilator and antihypertensive agent.
Features and Benefits
This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Bayer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Jennifer L Herington et al.
PloS one, 10(11), e0143243-e0143243 (2015-11-26)
The uterine myometrium (UT-myo) is a therapeutic target for preterm labor, labor induction, and postpartum hemorrhage. Stimulation of intracellular Ca2+-release in UT-myo cells by oxytocin is a final pathway controlling myometrial contractions. The goal of this study was to develop
Xue-yan Chen et al.
Yao xue xue bao = Acta pharmaceutica Sinica, 43(10), 1011-1018 (2009-01-09)
Effect of new calcium antagonist m-nisoldipine (m-Nis) on MCT-induced PH in rats and its mechanisms were investigated. Rats were injected with a single dose (60 mg x kg(-1)) of MCT subcutaneously to induce PH. Pulmonary haemodynamic measurement and lung tissue
Piero Ruggenenti et al.
Nature reviews. Nephrology, 6(6), 319-330 (2010-05-05)
Angiotensin II and other components of the renin-angiotensin-aldosterone system (RAAS) have a central role in the pathogenesis and progression of diabetic renal disease. A study in patients with type 1 diabetes and overt nephropathy found that RAAS inhibition with angiotensin-converting-enzyme
Tsuyoshi Shiga et al.
Heart and vessels, 22(6), 404-409 (2007-11-29)
The aim of this study was to investigate whether cilnidipine, an N- and L-type calcium channel blocker, and nisoldipine, an L-type calcium channel blocker, have different effects on sympathetic activity, using an identical group of healthy male subjects. Eight healthy
New Phenotypic Cytotoxicity Assay for ROS-inducing Compounds using Rat Renal Epithelial Cells
Uchiyama N, et al.
Toxicology Letters, 10(11) (2020)
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