Researchers at Lilly Research Laboratories in Indianapolis are studying a new SARM. It comes in the form of a gel that you can spread on your skin. The animal studies, which the researchers will soon publish in the Journal of Medicinal Chemistry, suggest that a daily application of just a few milligrams on your skin has an anabolic effect.
The full name of Eli Lilly’s new SARM is 2-chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile. A bit of a mouthful, so the researchers have named it compound 6 for the time being. Its structural formula is shown below. It’s surprisingly simple, which might mean that its productions costs are relatively low.
The researchers have presented the new compound specifically as a SARM that is suitable for transdermal use. The researchers spread compound 6 on the skin of deceased humans, and discovered that the stuff penetrated the skin just as well as good old testosterone does.
Attachment to steroid receptors
The researchers did in-vitro studies to determine how well compound 6 is capable of attaching itself to the androgen receptor [AR], the glucocorticoid receptor [the receptor for cortisol], the mineralocorticoid receptor [MR] and the progesterone receptor [PR]. They noticed that compound 6 only interacted with the androgen receptor and not with the other receptors.
Compound 6 did not attach itself as strongly to the androgen receptor as the killer steroid methyltrienolone does, but nevertheless it was pretty strong. By the way, compound 7 did even better in this respect.
Anabolic effect
Experiments with castrated rats revealed that transdermal administration of compound 6 in a daily dose of 0.3 mg per kg bodyweight was enough to maintain muscle mass [levator ani]. This dose of the new SARM performed as well as testosterone administered in a 10 mg dose of testosterone propionate per kg bodyweight daily.
Compound 6 had less effect on the prostate than testosterone does. That’s promising as this effect is an indicator of undesirable androgenic effects of androgenics-anabolic substances.
Human equivalent
For a man weighing 80 kg, the human equivalent of the dose tested for compound 6 would be about 3.5 mg daily, and for testosterone about 115 mg daily.
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy
Abstract
A transdermal SARM has a potential to have therapeutic benefit through anabolic activity in muscle while sparing undesired effects of benign prostate hyperplasia (BPH) and liver-mediated decrease in HDL-C. 2-Chloro-4-[(2-hydroxy-2-methyl-cyclopentyl)amino]-3-methyl-benzonitrile 6 showed the desired muscle and prostate effects in a preclinical ORX rat model. Compound 6 had minimal effect on HDL-C levels in cynomolgus monkeys and showed human cadaver skin permeability, thus making it an effective tool for proof-of-concept studies in a clinical setting.
Source: http://pubs.acs.org/doi/10.1021/acs.jmedchem.5b01168
