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SRT2183
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SRT2183图片
CAS NO:1001908-89-9
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)468.57
FormulaC27H24N4O2S
CAS No.1001908-89-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 93 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (6.4 mM)
Other info

Chemical Name: (R)-N-(2-(3-((3-hydroxypyrrolidin-1-yl)methyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-naphthamide

InChi Key: MUFSINOSQBMSLE-JOCHJYFZSA-N

InChi Code: InChI=1S/C27H24N4O2S/c32-22-11-12-30(15-22)14-21-17-34-27-29-25(16-31(21)27)23-7-3-4-8-24(23)28-26(33)20-10-9-18-5-1-2-6-19(18)13-20/h1-10,13,16-17,22,32H,11-12,14-15H2,(H,28,33)/t22-/m1/s1

SMILES Code: O=C(NC1=CC=CC=C1C2=CN3C(SC=C3CN4C[C@H](O)CC4)=N2)C5=CC=C6C=CC=CC6=C5

Synonyms

SRT2183; SRT 2183; SRT-2183.

实验参考方法
In Vitro

In vitro activity: SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. SRT2183 treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes. SRT1720, SRT2183, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. SRT2183 has little or no effect on SIRT1 deacetylating activity with native full-length substrates. SRT2183 activates AMPK, increases Sirt1 expression and decreases RelA/p65 lysine310 acetylation, critical for NF-κB activation, and an established Sirt1 target and inhibits RANKL-induced osteoclast generation and resorptive capacity in bone marrow macrophages.


Cell Assay: BMMs are harvested, plated and 24-hrs later non-adherent cells were re-plated at a density of 20,000 cells/well in α-MEM/15%FBS/5% M-CSF. For determining cell proliferation, cells are treated with SRT2183 or a vehicle for 72 hours post plating and BrdU reagent is added 48 hrs post SRT2183 or vehicle administration according to the manufacturer's instructions to determine cell proliferation 3 days post plating.

In Vivo
Animal model
Formulation & Dosage
References

Nature. 2007 Nov 29;450(7170):712-6; J Biol Chem. 2010 Mar 12;285(11):8340-51.