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N-氰基-N'-(1,1-二甲基丙基)-N''-(3-吡啶基)胍

用途

P-1075 是有效的、磺酰脲受体2相关的ATP敏感性的钾通道 (SUR2-KIR6)的激活剂,EC50 值为 45 nM。P-1075 还能在兔子中通过打开线粒体 K (ATP) 通道,产生活性氧,保护心脏。

名称

[ CAS 号 ]:
60559-98-0

[ 中文名 ]:
P-1075

[ 英文名 ]:
P1075

[英文别名 ]:

p-1075

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

EC50: 45 nM (SUR2-KIR6)[1].

[参考文献]

[1]. Schwanstecher M, et al. Potassium channel openers require ATP to bind to and act through sulfonylurea receptors. EMBO J. 1998 Oct 1;17(19):5529-35.

[2]. Oldenburg O, et al. P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts. J Mol Cell Cardiol. 2003 Sep;35(9):1035-42.

物理化学性质

[ 密度 ]:
1.07g/cm3

[ 沸点 ]:
347.6ºC at 760 mmHg

[ 熔点 ]:
186-187 °C

[ 分子式 ]:
C₁₂H₁₇N₅

[ 分子量 ]:
231.30

[ 闪点 ]:
164.1ºC

[ 精确质量 ]:
231.14800

[ PSA ]:
73.10000

[ LogP ]:
2.57268

[ 折射率 ]:
1.556

[ 储存条件 ]:
2-8°C，密封，干燥

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MF0175400

CHEMICAL NAME :: Guanidine, 2-cyano-1-tert-pentyl-3-(3-pyridyl)-

CAS REGISTRY NUMBER :: 60559-98-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C12-H17-N5

MOLECULAR WEIGHT :: 231.34

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 mg/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 21,773,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 21,773,1978

安全信息

[ 危害码 (欧洲) ]:
T+

[ 海关编码 ]:
2933399090

海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%