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Merck
CN
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文件

475840

Sigma-Aldrich

米力农

A cell-permeable, selective inhibitor of cGMP-inhibited phosphodiesterase (PDE III; IC₅₀ = 300 nM).

别名:

米力农, 1,6-二氢-2-甲基-6-氧-(3,4ʹ-联吡啶)-5-甲腈

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About This Item

经验公式(希尔记法):
C12H9N3O
CAS号:
分子量:
211.22
MDL编号:
UNSPSC代码:
12352200

质量水平

检测方案

≥99% (HPLC)

形式

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze

颜色

white

溶解性

DMSO: 20 mg/mL
ethanol: 3 mg/mL

运输

ambient

储存温度

−20°C

InChI

1S/C12H9N3O/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8/h2-6H,1H3,(H,15,16)

InChI key

PZRHRDRVRGEVNW-UHFFFAOYSA-N

一般描述

cGMP抑制的磷酸二酯酶(PDE III;IC50 =300 nM)的细胞可渗透的选择性抑制剂。对心脏有正性变时性、变力性和血管舒张作用。
cGMP抑制的磷酸二酯酶(PDE III;IC50 =300 nM)的细胞可渗透的选择性抑制剂。对心脏有正性变时性、离子移变性和血管舒张作用。

生化/生理作用

主要靶标
PDE 3
产物不与ATP竞争。
可逆:否
细胞可渗透性:具有
靶标IC50:PDE III为300 nM

警告

毒性:有毒(F)

重悬

溶解后,等分并冷冻保存(-20°C)。储备溶液在-20°C下可稳定保存2个月。

其他说明

Bailey, J.M., et al. 1994.Anesthesiology 81, 616.
Wilhelm, D., et al. 1992.J. Cardiovasc.Pharmacol.20, 705.
Lindgren, S.H., et al. 1990.Acta.Phys.Scand.140, 209.
Harrison, S.A., et al. 1986.Mol.Pharmacol.29, 506.
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法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

象形图

Skull and crossbones

警示用语:

Danger

危险声明

危险分类

Acute Tox. 3 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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J M Bailey et al.
Anesthesiology, 81(3), 616-622 (1994-09-01)
Milrinone is a phosphodiesterase inhibitor with positive inotropic and vasodilator effects that are useful in the treatment of ventricular dysfunction after cardiac surgery. However, the pharmacokinetics of the drug have been investigated only in healthy volunteers and in patients with
S H Lindgren et al.
Acta physiologica Scandinavica, 140(2), 209-219 (1990-10-01)
The inhibitors of the cGMP-inhibited, low-Km cAMP phosphodiesterase--milrinone and OPC 3911--and an inhibitor of a non-cGMP-inhibited low-Km cAMP phosphodiesterase--rolipram--were used to evaluate the functional importance of the two cAMP phosphodiesterase activities in vascular smooth muscle and in platelets. Vinpocetine, an
S A Harrison et al.
Molecular pharmacology, 29(5), 506-514 (1986-05-01)
We have identified and highly purified a "low Km" cAMP phosphodiesterase from bovine cardiac muscle. This phosphodiesterase was inhibited by low concentrations of cGMP and has, therefore, been temporarily designated as cGMP-inhibited phosphodiesterase. After a 16,000-fold increase in specific activity
D Wilhelm et al.
Journal of cardiovascular pharmacology, 20(5), 705-714 (1992-01-01)
The cardiac in vitro effects of R 80122, a novel phosphodiesterase (PDE) inhibitor, were investigated and compared with those of the reference compound milrinone and of the calcium-sensitizer adibendan. In guinea pig left atria, both milrinone and R 80122 increased
Luping Yu et al.
Development (Cambridge, England), 148(2) (2020-12-16)
Alternative splicing (AS) contributes to gene diversification, but the AS program during germline development remains largely undefined. Here, we interrupted pre-mRNA splicing events controlled by epithelial splicing regulatory protein 1 (ESRP1) and found that it induced female infertility in mice.

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