SRT2104 (GSK2245840)

Biological Activity

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.