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) |
|---|
依拉地平, Ca v1.2的门控抑制剂;Ca v1.3的门控抑制剂;Ca v1.4的门控抑制剂
有货
概述
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drμgs/Drμg CandidatesIsradipine has been used to explore neuroprotective activity.
Information
Isradipine Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.
In vitro
Isradipine produces inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. Isradipine is found to be the most potent derivative in both, in growth cultures (I50 = 20.8 mM) and in vivo oxygen uptake (I50 = 31.1 mM).
In vivo
Isradipine reduces hypoxia-induced activation of calcium dependent xanthine oxidases, monoamine oxidases, cytosolic phospholipase A(2) and cyclooxygenases (COX-2) along with concomitant decrease in free radical generation and cytochrome c release. Isradipine prevents hypobaric hypoxia along with augmented neurodegeneration and memory impairment induced increased expression of calpain and caspase 3. Isradipine (at the dose of 1 mg/kg three times a day) reduces ethanol intake by over 70% in ethanol-preferring rats, the reduction in ethanol intake is compensated by a proportional increase in water consumption and the inhibitory effect persisted throughout the 5 days of treatment. Isradipine significantly reduces the arterial wall collagen contents in both strains, with marked increases in the elastin content in the carotid but not in the aortic wall in spontaneously hypertensive rats. Isradipine suppresses the reinforcing properties of morphine and cocaine and may be an effective pharmacotherapy for treatment of cocaine and heroin abuse in mice.
Cell Data
cell lines：MCSF-dependent mouse myeloid M-NFS-60 cell line
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Isradipine
生化机理
伊斯拉地平（PN 200-110）是一种强效的选择性 L 型电压门控钙通道阻滞剂，用于治疗高血压。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
门控抑制剂
作用机制
Ca v1.2的门控抑制剂;Ca v1.3的门控抑制剂;Ca v1.4的门控抑制剂
名称和识别符
EC号
630-420-5
分子类型
小分子
Isomeric SMILES
CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC
分子量
371.39
Reaxy-Rn
6576633
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6576633&ln=
高级数据
关联靶点（人）
CACNA1C
Tclin
电压依赖性 L 型钙通道亚基 α-1C(Voltage-dependent L-type calcium channel subunit alpha-1C)
(4 活性数据)
CACNA1D
Tclin
电压依赖性 L 型钙通道亚基 alpha-1D(Voltage-dependent L-type calcium channel subunit alpha-1D)
(1 活性数据)
CACNA1F
Tchem
电压依赖性 L 型钙通道亚基 α-1F(Voltage-dependent L-type calcium channel subunit alpha-1F)
(1 活性数据)
化学和物理性质
熔点
169 °C
安全和危险性（GHS）
信号词
危险
危险声明
H319: 引起严重眼睛刺激
H301: 吞咽会中毒
H400: 对水生生物毒性极大
H410: 对水生生物毒性极大并具有长期持续影响
H372: 长期或反复接触会对器官造成损害
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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。
P321: 特殊处理（请参阅此标签上的...）。
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
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P301+P316: 如果吞咽：立即寻求紧急医疗救助。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
P319: 如果你感到不适，请寻求医疗帮助。
WGK Germany
3
Merck Index
5240
个人防护装备
Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter
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
溶液计算器
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危险品化学品经营许可证（带存储）