NKY80

NKY80用途

NKY80 是一种有效的,选择性和非竞争性的 V 型腺苷酸环化酶 (AC) 异构体抑制剂,对于 V 型,III 型和 II 型,IC50 分别为 8.3 µM,132 µM 和 1.7 mM。NKY80 是一种非核苷的喹唑啉酮,可调节心脏和肺组织中的 AC 催化活性。

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NKY80名称

[ CAS 号 ]:
299442-43-6

[ 中文名 ]:
2-氨基-7-呋喃-2-基-7,8-二氢-6H-喹唑啉-5-酮

[ 英文名 ]:
NKY 80

[英文别名 ]:

BCX 34
PELDESINE
Peldesine

NKY80生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷酸环化酶

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: 8.3 µM (AC type V), 132 µM (AC type III) and 1.7 mM (AC type II)[1]

[体外研究]

NKY80(20μM)阻断了最大浓度(10nm)引起的左室压和心室cAMP水平的升高[2]。NKY80(20μM；2小时)完全阻断了JG细胞cAMP含量和肾素释放的增加[3]。

[参考文献]

[1]. Onda T, et al. Type-specific regulation of adenylyl cyclase. Selective pharmacological stimulation and inhibitionof adenylyl cyclase isoforms. Biol Chem. 2001 Dec 21;276(51):47785-93.

[2]. Harney JA, et al. Insulin-like stimulation of cardiac fuel metabolism by physiological levels of glucagon: involvement of PI3K but not cAMP. Am J Physiol Endocrinol Metab. 2008 Jul;295(1):E155-61.

[3]. Ortiz-Capisano MC, et al. Adenylyl cyclase isoform v mediates renin release from juxtaglomerular cells. Hypertension. 2007 Mar;49(3):618-24.

NKY80物理化学性质

[ 分子式 ]:
C₁₂H₁₁N₃O₂

[ 分子量 ]:
229.23500

[ 精确质量 ]:
229.08500

[ PSA ]:
82.01000

[ LogP ]:
2.14570

[ 储存条件 ]:
2-8°C

NKY80MSDS

详细MSDS(安全技术说明书)

NKY80安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
T

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

[ 海关编码 ]:
2934999090

NKY80海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

NKY80文献

Late INa increases diastolic SR-Ca2+-leak in atrial myocardium by activating PKA and CaMKII.

Cardiovasc. Res. 107 , 184-96, (2015)

Enhanced cardiac late Na current (late INa) and increased sarcoplasmic reticulum (SR)-Ca(2+)-leak are both highly arrhythmogenic. This study seeks to identify signalling pathways interconnecting late ...

In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.

Proc. Natl. Acad. Sci. U. S. A. 105 , 9059-64, (2008)

The growing resistance to current first-line antimalarial drugs represents a major health challenge. To facilitate the discovery of new antimalarials, we have implemented an efficient and robust high-...

Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.

Science 334 , 1372-7, (2011)

Most malaria drug development focuses on parasite stages detected in red blood cells, even though, to achieve eradication, next-generation drugs active against both erythrocytic and exo-erythrocytic f...

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