N-氰基-N'-(1,1-二甲基丙基)-N''-(3-吡啶基)胍

• 常用名: N-氰基-N'-(1,1-二甲基丙基)-N''-(3-吡啶基)胍
• 英文名: P1075
• CAS号: 60559-98-0
• 分子量: 231.30
• 密度: 1.07g/cm3
• 沸点: 347.6ºC at 760 mmHg
• 分子式: C₁₂H₁₇N₅
• 熔点: 186-187 °C
• 闪点: 164.1ºC

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

• 中文名: P-1075
• 英文名: 1-cyano-2-(2-methylbutan-2-yl)-3-pyridin-3-ylguanidine

生物活性

• 描述: 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。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 靶点实验:

  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
• InChIKey: HKZNADVVGXKQDL-UHFFFAOYSA-N
• SMILES: CCC(C)(C)N=C(NC#N)Nc1cccnc1
• 折射率: 1.556
• 储存条件: 2-8°C， 密封， 干燥

毒性和生态

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%

靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro... 来源：NCGC 靶标：N/A External Id：SERCaMPGLuc-p1-antagonist

实验名称：Vasorelaxant activity in rat bladder assessed as inhibition of carbachol-induced cont... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL1006155

实验名称：Selectivity ratio of EC50 for african green monkey SUR2A/Kir6.2 potassium ATP channel... 来源：ChEMBL 靶标：N/A External Id：CHEMBL1006154

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020);... 来源：ChEMBL 靶标：Staphylococcus aureus External Id：CHEMBL4296184

实验名称：Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1315

实验名称：Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); ... 来源：ChEMBL 靶标：Klebsiella pneumoniae External Id：CHEMBL4296186

实验名称：Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CA... 来源：ChEMBL 靶标：Escherichia coli External Id：CHEMBL4296185

实验名称：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

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英文别名

• p-1075