testolone-rad140

Description: Testolone (formerly known as RAD140) is a novel, potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that is being investigated for the treatment of conditions such as muscle wasting and breast cancer. RAD140 is also neuroprotective in cultured neurons and kainate-lesioned male rats. In cultured hippocampal neurons, RAD140 was as effective as testosterone in reducing cell death induced by apoptotic insults. Mechanistically, RAD140 neuroprotection was dependent upon MAPK signaling, as evidenced by elevation of ERK phosphorylation and inhibition of protection by the MAPK kinase inhibitor U0126. Importantly, RAD140 was also neuroprotective in vivo using the rat kainate lesion model.

References: ACS Med Chem Lett. 2010 Dec 2; 2(2):124-9; Endocrinology. 2014 Apr; 155(4):1398-406.