化合物SRT2183 | 1001908-89-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: 化合物SRT2183
• 英文名称: (R)-N-(2-(3-((3-hydroxypyrrolidin-1-yl)methyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-naphthamide
• 英文别名: N-[2-[3-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]naphthalene-2-carboxamide
• CAS: 1001908-89-9
• 化学式: C₂₇H₂₄N₄O₂S
• 分子量: 468.6
• InChiKey: MUFSINOSQBMSLE-JOCHJYFZSA-N

物化性质

• 溶解度：
  DMSO：250 mg/mL（533.54 mM；需要超声波）

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  98.1
• 氢给体数：
  2
• 氢受体数：
  5

制备方法与用途

生物活性

SRT2183是sirtuin蛋白亚型SIRT1的小分子激活剂。

靶点

Target	Value
SIRT1

体外研究

1-20 μM SRT2183 能有效抑制细胞生长和凋亡。它能引起促凋亡、生长停滞、DNA损伤反应相关基因的mRNA水平提高。SRT1720, SRT2183, SRT1460和resveratrol对一些受体、酶、转运体和离子通道有多种脱靶作用。它们并不是SIRT1的直接激活剂。SRT2183对SIRT1去乙酰化活性没有或者有很小的作用。SRT2183激活AMPK、增加Sirt1的表达、降低RelA/p65第310位赖氨酸的乙酰化水平，对NF-κB的激活、Sirt1靶标的建立有关键作用、在骨髓巨噬细胞中，抑制RANKL诱导的破骨细胞生成和再吸收能力。

文献信息

• COMPOSITIONS AND METHODS FOR MODULATING METABOLIC PATHWAYS
  申请人：NuSirt Sciences, Inc.

  公开号：EP3466418A1

  公开（公告）日：2019-04-10

  Compositions and methods useful for inducing an increase in fatty acid oxidation or mitochondrial biogenesis, reducing weight gain, inducing weight loss, or increasing Sirt1, Sirt3, or AMPK activity are provided herein. Such compositions can contain synergizing amounts of a sirtuin-pathway activators, including but not limited to resveratrol, in combination with beta-hydroxymethylbutyrate (HMB), keto isocaproic acid (KIC), leucine, or combinations of HMB, KIC and leucine.

  本文提供了有助于诱导脂肪酸氧化或线粒体生物生成增加、减少体重增加、诱导减肥或增加 Sirt1、Sirt3 或 AMPK 活性的组合物和方法。此类组合物可含有协同增效量的sirtuin-途径激活剂，包括但不限于白藜芦醇，与β-羟甲基丁酸（HMB）、酮异己酸（KIC）、亮氨酸或HMB、KIC和亮氨酸的组合物结合使用。
• Compositions and methods for modulating metabolic pathways
  申请人：NuSirt Sciences, Inc.

  公开号：US10383837B2

  公开（公告）日：2019-08-20

  Compositions and methods useful for inducing an increase in fatty acid oxidation or mitochondrial biogenesis, reducing weight gain, inducing weight loss, or increasing Sirt1, Sirt3, or AMPK activity are provided herein. Such compositions can contain synergizing amounts of a sirtuin-pathway activators, including but not limited to resveratrol, in combination with beta-hydroxymethylbutyrate (HMB), keto isocaproic acid (KIC), leucine, or combinations of HMB, KIC and leucine.

  本文提供了有助于诱导脂肪酸氧化或线粒体生物生成增加、减少体重增加、诱导减肥或增加 Sirt1、Sirt3 或 AMPK 活性的组合物和方法。此类组合物可含有协同增效量的sirtuin-途径激活剂，包括但不限于白藜芦醇，与β-羟甲基丁酸（HMB）、酮异己酸（KIC）、亮氨酸或HMB、KIC和亮氨酸的组合物结合使用。
• Method for treating benign prostate hyperplasia using resveratrol
  申请人：Leheste Joerg R.

  公开号：US20100048577A1

  公开（公告）日：2010-02-25

  The invention relates to the discovery that resveratrol, and substituted forms of resveratrol, are effective in alleviating benign prostate hyperplasia. Formulations containing the resveratrol or resveratrol derivative, lack omega-3 fatty acids, and also contain no other compounds which activate SIRT1 and PGCα.
• Use of SIRT1 Activators or Inhibitors to Modulate an Immune Response
  申请人：VERDIN ERIC M.

  公开号：US20100330114A1

  公开（公告）日：2010-12-30

  The present disclosure provides a method of increasing an immune response in an individual, the method involving administering to an individual in need thereof an inhibitor of SIRT1. The present disclosure provides a method of reducing an immune response, e.g., to treat chronic immune hyperactivity, the method generally involving administering to an individual in need thereof an activator of SIRT1. The present disclosure provides a method of modulating activation and differentiation of CD4 + T cells.
• COMPOSITIONS AND METHODS RELATED TO SIRT1 FUNCTION
  申请人：Sassone-Corsi Paolo

  公开号：US20110269817A1

  公开（公告）日：2011-11-03

  The invention relates to modulation of circadian rhythm and underlying biological processes.