切换导航

SRT2104 (GSK2245840)

现货
Catalog No.
A3821
SIRT1激活剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,050.00
现货
25mg
¥ 3,350.00
现货
100mg
¥ 6,990.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. SIRT1, also known as NAD-dependent deacetylase sirtuin-1, is a member of the sirtuin family of proteins.

In vitro: In C2C12 myoblasts stably transfected with small hairpin RNA to knock-down SIRT1, SRT2104 increased AP activity, a marker for osteogenic differentiation. This effect was totally dependent on SIRT1 expression [1].

In vivo: In male C57BL/6J mice, administration of SRT2104 (100 mg/kg, p.o.) extended both mean and maximal lifespan of mice fed a standard diet, and enhanced bone mineral density, motor coordination, and insulin sensitivity and decreased inflammation. Short-term SRT2104 administration preserved bone and muscle mass in an experimental model of atrophy [1]. In Male N171-82Q HD mice with Huntington's disease, SRT2104 (diet containing 0.5% SRT2104) effectively penetrated the blood-brain barrier, attenuated brain atrophy, improved motor function, and extended survival [2].

References:
[1].  Mercken E M, Mitchell S J, Martin‐Montalvo A, et al. SRT2104 extends survival of male mice on a standard diet and preserves bone and muscle mass[J]. Aging Cell, 2014, 13(5): 787-796.
[2].  Jiang M, Zheng J, Peng Q, et al. Sirtuin 1 activator SRT2104 protects Huntington's disease mice[J]. Annals of clinical and translational neurology, 2014, 1(12): 1047-1052.

文献引用

1. Dai Y, Chen T, et al. "SIRT1 activates the expression of fetal hemoglobin genes." Am J Hematol. 2017 Aug 4. PMID:28776729

Chemical Properties

StorageStore at -20°C
M.Wt516.64
Cas No.1093403-33-8
FormulaC26H24N6O2S2
Solubility≥6.46 mg/mL in DMSO with gentle warming, <2.55 mg/mL in EtOH, <2.4 mg/mL in H2O
Chemical Name4-methyl-N-[2-[3-(morpholin-4-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-pyridin-3-yl-1,3-thiazole-5-carboxamide
SDFDownload SDF
Canonical SMILESCC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

C2C12成肌细胞

溶解方法

可溶于DMSO。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

3 μM,24 h

应用

在稳定转染小发卡RNA来敲减SIRT1的C2C12成肌细胞中,SRT2104增加AP活性,即成骨分化的标志物,这种作用完全依赖SIRT1表达。SRT2104增加线粒体含量,抑制炎症反应。

动物实验 [1]:

动物模型

雄性C57BL/6J小鼠

给药剂量

口服,100 mg/kg,6周

应用

在雄性C57BL/6J小鼠中,SRT2104(100 mg/kg, p.o.)治疗改善了全身生理学,并延长了使用标准饮食的小鼠的寿命,增加了骨矿物质密度、运动协调和胰岛素敏感性,减少了炎症反应。在萎缩实验模型中,短期给药SRT2104保存了骨骼和肌肉质量。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Mercken E M, Mitchell S J, Martin‐Montalvo A, et al. SRT2104 extends survival of male mice on a standard diet and preserves bone and muscle mass[J]. Aging Cell, 2014, 13(5): 787-796.

质量控制

化学结构

SRT2104 (GSK2245840)

相关生物数据

SRT2104 (GSK2245840)