The majority, according to what you posted, is excreted as deoxyecdysone. I'm not sure how this is proof it's not entering muscle tissue.
The study I posted showed that it is excreted in much higher levels as Ecdysterone than Deoxyecdysone (I have only had time to skim these...I may be misinterpreting so if I am, I will concede).
Looks like the hydroxyl group at C22 is conjugated pretty easily and that conjugate is excreted.
So, it is a solubility issue but not of Ecdy itself but rather of it's metabolite. Since these conjugations tend to happen in 1st pass I stand by our earlier conclusion of poor oral bioavailability.
With this in mind it makes sense that other conditions in the gut could effect absorption, ie empty stomach vs taking it with a fatty meal, etc.
If this was a first pass (or any) conjugation issue, higher doses would eventually exhaust this mechanism and the study at hand contradicts this - the high dose group didn't do as well as the lower dose group.
It was less than 1% of the original ecdy excreted un-metabolized, so it should be lipophilic enough to pass a cell wall before being conjugated. Just too much is getting conjugated before it gets that chance. This makes sense based on the myotube studies as well.
Maybe I'll make a small batch of TD.
Again, if it were just conjugation - high dose and/or chronic administration would show better results, and this does not appear to be the case?
480-ish. That isn't an issue.
LogP = - .5 or so -- so polar, but not problematically so for cellular uptake.
Not ideal for transdermal at all, but not overwhelmingly so. But, it could get expensive, especially if it is being metabolized, heavily, in tissues other than the liver.
Powercage seems to be indicating that the metabolism is maybe in the blood itself, or at some other point? It just does not get into the muscles...but I'm not sure if that is an issue either. I mean, we're dealing with an insect signaling hormone here...it may be a cascade more than a direct effect.
For further discussion:
Ecdysone is an arthropod molting hormone and has been marketed as a non-androgenic natural anabolic and adaptogen. However, the safety profile of ecdysone is largely undetermined. After ecdysone treatment for 2 weeks, mice developed albuminuria with histologic signs of glomerular injury...
www.nature.com
Ecdysone does not appear to be the same chemical - but is extremely similar and the second study I posted does seem to indicate some ecdysterone gets metabolized into ecdysone.
Yes, please do. If this is a real risk with ecdysterone I’d like to know because at this point, I really do plan on it running it 8-12 weeks on followed by 2-3 weeks off forever.
I feel great on it.
Again, if bioavailability is an issue because of conjugation - long-term use may be a way to overcome the issue. THIS may be a factor in why some people respond better than others - they can afford a relatively expensive ingredient for a longer run at a higher dose. It may be that by weeks 4-6 you are starting to exhaust the machinery needed to conjugate this compound, and some people may hit that point in 2 weeks or something.
Still - the conjugation theory, in my mind and I could be wrong, seems to be contradicted in the study, because the higher dose group didn't do any better - whatever bio availability issues there are, a higher dose should still yield more getting through in most cases.