Hyperanabolic SARM Found

CDB

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Swiped this from Lyle's Body Recomposition board. Some good discussion and references on this and other SARMs going on there.

Endocrinology. 2007 Jan;148(1):4-12. Epub 2006 Sep 28.

Comment in:
Endocrinology. 2007 Jan;148(1):1-3.

Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.

* Ostrowski J,
* Kuhns JE,
* Lupisella JA,
* Manfredi MC,
* Beehler BC,
* Krystek SR Jr,
* Bi Y,
* Sun C,
* Seethala R,
* Golla R,
* Sleph PG,
* Fura A,
* An Y,
* Kish KF,
* Sack JS,
* Mookhtiar KA,
* Grover GJ,
* Hamann LG.

Department of Metabolic Diseases, Bristol-Myers Squibb, Pharmaceutical Research Institute, Princeton, NJ 08543, USA.

A novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (BMS-564929) has been identified, and this compound has been advanced to clinical trials for the treatment of age-related functional decline. BMS-564929 is a subnanomolar AR agonist in vitro, is highly selective for the AR vs. other steroid hormone receptors, and exhibits no significant interactions with SHBG or aromatase. Dose response studies in castrated male rats show that BMS-564929 is substantially more potent than testosterone (T) in stimulating the growth of the levator ani muscle, and unlike T, highly selective for muscle vs. prostate. Key differences in the binding interactions of BMS-564929 with the AR relative to the native hormones were revealed through x-ray crystallography, including several unique contacts located in specific helices of the ligand binding domain important for coregulatory protein recruitment. Results from additional pharmacological studies effectively exclude alternative mechanistic contributions to the observed tissue selectivity of this unique, orally active androgen. Because concerns regarding the potential hyperstimulatory effects on prostate and an inconvenient route of administration are major drawbacks that limit the clinical use of T, the potent oral activity and tissue selectivity exhibited by BMS-564929 are expected to yield a clinical profile that provides the demonstrated beneficial effects of T in muscle and other tissues with a more favorable safety window.

PMID: 17008401 [PubMed - indexed for MEDLINE]
 
wastedwhiteboy2

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I'm interested in hearing more about this.
 
CDB

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I'm interested in hearing more about this.
Head over to the recomp boards at McDonald's site. Dan, the guy who runs the hypertrophy research site in my sig, posted a boatload of studies and there's some discussion going on about them.
 
rms80

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Swiped this from Lyle's Body Recomposition board. Some good discussion and references on this and other SARMs going on there.
Good post!!
 
LakeMountD

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I have mentioned this before. The synthesis for most of the ones we looked into were over $100,000 for 100 grams.
 
CDB

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I have mentioned this before. The synthesis for most of the ones we looked into were over $100,000 for 100 grams.
That's officially a ****load of money. I'll wait for the black market.
 
LakeMountD

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That's officially a ****load of money. I'll wait for the black market.
Haha it will be a while. The only reason it is so expensive is because it isn't mass produced like say test. I'm sure it will take a good 7 years or more before we start seeing these things on the street.

That is just a guess though, depends on how they do in clinical studies, side effects, etc.
 
bioman

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Oh yeah, that formula will definitely find it's way into some labs in China.

I wonder if this SARM also attaches to heart muscle. If it doesn't then it could well be the perfect muscle builder.
 
LakeMountD

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Oh yeah, that formula will definitely find it's way into some labs in China.

I wonder if this SARM also attaches to heart muscle. If it doesn't then it could well be the perfect muscle builder.
From the studies I remember reading, it only attached to bone and skeletal muscle, which is pretty crazy.
 
UnicronSpawn

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Man, I can hardly wait to see the day when the new SARMS are mass produced and the price becomes reasonable. Exciting stuff.
 
Jayhawkk

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Damn that's a nice find CDB. I have to spread it around again >< :)
 
LakeMountD

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Damn that's a nice find CDB. I have to spread it around again >< :)
Geez why didn't I get any rep when I posted this months ago?! lol. We were actually looking into it for quite some time but no matter where we looked it was just ridiculously priced. I think it is the synthesis, could just be expensive starting materials or something. I didn't really look too much at structure but the name was long.
 
Jayhawkk

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Hey, i'm only human :) Maybe you didn't word it as pretty, lol
 

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