Testolone RAD-140

RAD-140, or (2-chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino] -3-methylbenzonitrile, also known as testolone, was originally synthesized for Radius Health Inc. in collaboration with researchers from the University of Illinois, Obiter Research and Cambridge Major Laboratories.

According to the first paper describing the synthesis and preliminary findings of the compound, RAD140 has stability up to (t1/2 > 2 h) in incubations with rat and monkey microsomes, as well as high affinity for the androgen receptor (Ki = 7 nM ), about 4 times the affinity than that of testosterone itself. At the same time, the closest hormone receptor activated by RAD140 was progesterone at a level of 750 nM.

The earliest primate studies on RAD-140 indicated that even at the lowest dose range of 0.1 mg/kg, juvenile macaques gained an average of ten percent in body weight during the 28-day trial, mostly confirmed to be lean body mass. however, through DEXA scans performed before and after the trial period, this was somewhat variable.

Currently, RAD-140 has potential for future research efforts in neuromodulation, as it was shown to have protective properties in the brains of rats that had reduced androgen levels.

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Data Sheet

RAD140 (Testolone)