Sipasterol

Sipasterol (5α-Androstane-3β,5,6β-triol) is a neuroprotectant. Sipasterol can remarkably reverse intracellular acidification and alleviate neuronal injury through the inhibition of AMPK signaling. Sipasterol remarkably reduced the infarct volume and attenuated neurologic impairment in acute ischemic stroke models of middle cerebral artery occlusion in vivo^[1]. IC50 & Target:AMPK^[1] In Vitro:Sipasterol (TRIOL) (10 μM; for 35 min) inhibits the enhanced phosphorylation of neuronal AMPK caused by glutamate. Sipasterol also significantly attenuates the enhanced glycolysis and intracellular lactate accumulation^[1].
Sipasterol (10 μM; for 35 min) significantly blocks the increase in terminal deoxynucleotidyl transferase dUTP nick-end labeling TUNEL-positive cells and the ratio of cleaved caspase-3/caspase-3 induced by glutamate^[1].
In Vivo:Sipasterol (TRIOL) (1-20 mg/kg; intraperitoneal injection; single dose) dose dependently protects C57BL/6 mice against brain injury caused by permanent focal cerebral ischemia. Sipasterol dose dependently protects SD rats against brain injury induced by transient focal cerebral ischemia^[1].