SRT2104 is a selective brain-permeable activator of SIRT1. SRT2104 (3 μM) reduces p65/RelA acetylation levels in C2C12 cells.
In vivo, SRT2104 (100 mg/kg, p.o.) improves whole-body physiology and extends lifespan in mice fed a standard diet. SRT2104 increases mitochondrial content and suppresses the inflammatory response in SD-fed mice. In Male N171-82Q HD mice, SRT2104 (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival.
| Molecular Weight | 516.64 |
| Formula | C26H24N6O2S2 |
| CAS Number | 1093403-33-8 |
| Solubility (25°C) | DMSO: 5 mg/mL (Need ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Fuzhe Ma, et al. P53/NRF2 mediates SIRT1's protective effect on diabetic nephropathy
[5] Jos M Villalba, et al. Sirtuin activators and inhibitors
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