PNU 37883 hydrochloride

• 常用名: PNU 37883 hydrochloride
• 英文名: U-37883A
• CAS号: 57568-80-6
• 分子量: 381.98300
• 密度: N/A
• 沸点: 474.1ºC at 760mmHg
• 分子式: C₂₁H₃₆ClN₃O
• 熔点: N/A
• 闪点: 240.5ºC

PNU 37883 hydrochloride用途

PNU 37883盐酸盐(PNU 37883A)是一种选择性血管ATP敏感性钾(Kir6,KATP)通道阻滞剂。PNU 37883盐酸盐具有利尿作用,在肾脏和血管平滑肌中具有特异性结合,而不是在大脑或胰腺β细胞中[1][2]。

PNU 37883 hydrochloride名称

• 英文名: N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide,hydrochloride

PNU 37883 hydrochloride生物活性

• 描述: PNU 37883盐酸盐(PNU 37883A)是一种选择性血管ATP敏感性钾(Kir6,KATP)通道阻滞剂。PNU 37883盐酸盐具有利尿作用,在肾脏和血管平滑肌中具有特异性结合,而不是在大脑或胰腺β细胞中[1][2]。
• 相关类别:
  研究领域 >> 神经疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 体外研究: 在稳定表达Kir6.2/SUR1、Kir6.2/SUR2A、Kir6.2/SUR2B或Kir6.1/SUR2B的HEK-293细胞中,PNU-37883A抑制四种类型的KATP通道,但程度不同。抑制假定的平滑肌KATP通道类型,Kir6.2/SUR2B(IC50为15μM)和Kir6.1/SUR2B(IC50为6μM)。PNU-37883A显著抑制单独表达Kir6.2Δ26产生的电流,IC50为5μM,当用SUR2B表达Kir6.2Δ26时,IC50显著增加至38μM[1]。PNU 37883(0.1-10 nM)盐酸盐在苯肾上腺素或KCl预收缩主动脉环中产生浓度依赖性胍丁胺(100μM)松弛衰减。然而,单独使用PNU 37883(10 nM)盐酸盐治疗不会改变血管张力[3]。
• 参考文献:

  [1]. Yi Cui, et al. Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A. Br J Pharmacol. 2003 May;139(1):122-8.

  [2]. Noriyoshi Teramoto. Pharmacological Profile of U-37883A, a Channel Blocker of Smooth Muscle-Type ATP-Sensitive K Channels. Cardiovasc Drug Rev. Spring 2006;24(1):25-32.

  [3]. Guang-Yuan Mar, et al. Changes of imidazoline receptors in spontaneously hypertensive rats. Int J Exp Pathol. 2013 Feb;94(1):17-24.

PNU 37883 hydrochloride物理化学性质

• 沸点: 474.1ºC at 760mmHg
• 分子式: C₂₁H₃₆ClN₃O
• 分子量: 381.98300
• 闪点: 240.5ºC
• 精确质量: 381.25500
• PSA: 36.86000
• LogP: 4.69650
• InChIKey: FZALCKUJYZCDOX-UHFFFAOYSA-N
• SMILES: C1CCC(N=C(NC23CC4CC(CC(C4)C2)C3)N2CCOCC2)CC1.Cl

PNU 37883 hydrochloride安全信息

• 安全声明 (欧洲): 22-24/25

PNU 37883 hydrochloride靶点实验

查看更多实验

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：qHTS for Inhibitors of Polymerase Iota 来源：NCGC 靶标：DNA polymerase iota [Homo sapiens] External Id：PolI100

实验名称：qHTS for Inhibitors of Polymerase Eta 来源：NCGC 靶标：DNA polymerase eta [Homo sapiens] External Id：PolE100

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Small-molecule inhibitors of ST2 (IL1RL1) 来源：20881 靶标：interleukin-1 receptor-like 1 isoform [homo sapiens] External Id：ST2_IL33_Inhibitors_Primary_Screening_77700

实验名称：qHTS Assay for Small Molecule Inhibitors of the Human hERG Channel Activity 来源：NCGC External Id：HERG01

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

实验名称：qHTS Assay for Inhibitors of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1):... 来源：NCGC 靶标：thioredoxin reductase [Rattus norvegicus] External Id：TRXR100

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

共24条，当前第1页，共3页

1

2

3

PNU 37883 hydrochloride英文别名

• 4-Morpholinecarboximidine-N-1-adamantyl-N'-cyclohexane