Cost is in the first post of this thread. But you have to work in a lab to order it.
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Alfatradiol (17-alpha estradiol) is marketed under the brand names Avicis, Avixis, Ell-Cranell Alpha, and Pantostin. In Pantostin, it is dissolve in propan-2-ol ( Isopropyl alcohol ), a toxic compound. At ambiant temperature, Isopropyl alcohol evaporates. Inhalation of the vapors can also be toxic. My understanding is that 17-alpha estradiol do not evaporate in this process. There is 0,25mg of alfatradiol per ml of solution.
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Yes - but this is topical use, not the systemic use like in the NIA ITP program that resulted in the mice living much longer.
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Some info from another doctor I know who’s been looking into 17-alpha estradiol:
I know 17bE2 is practically insoluble in water, so I was originally looking into using extra virgin olive oil (or maybe MCT oil + antioxidant might be better since EVOO is much more “fragile”) with a dark bottle and oxygen absorber, which would take out the oxygen that could degrade the 17aE2 in presence of light/UV. Then one could add say lauroyl macroglycerides as surfactant, lecithin as homogenizer, and finally optional cosolvent like glycerol. This is just to make sure it is homogeneous and doesn’t precipitate at all over say a few months - which could mess up with dosing. Have the study on hand for 17aE2 aqueous solution?
17aE2 is even stable while heating vegetable oil at 100 C.
Effect of cooking on concentrations of β-estradiol and metabolites in model matrices and beef - PubMedI’d also point out sublingual option could save at ~1/5 the cost, since it would probably be much more expensive if more pure though - so savings without user error like injections would probably make it more available to everyone if they end up charging say 5x the price for 10 gram “wholesale” which could be $3k a year per oral.
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In the long-term we males who are interested in using 17-alpha estradiol are going to want to make sure there is very low levels of 17-beta estradiol (the feminizing hormone typically used in hormone replacement therapy by women).
So the issue of testing comes up when thinking about this drug. Specifically, testing for the percent of alpha vs. beta estradiol in the product you are buying.
Some of the conversation on this topic:
The problem is I wonder how they claim to do it purity-wise. Sounds like they want to keep the process hush. Been a while since I did a wet lab in organic synthesis for ligand synthesis, so I’d have to dust off some old O chem and A chem books. I suspect 99%+ enantiomer selectivity should be possible though and should be easy to use a tiny amount to send out for a ng/mL sample in a lab for HPLC-UV to test for their claim of essentially 100% purity. Was wondering what your chem professor thought, if he’s willing to comment.
and the response from my Chem professor friend:
Shouldn’t need too much sample to conduct the test.
However, diastereomers can be difficult to separate, even by HPLC. The lab may require some background work unless there is an available SOP for a- and b- estradiol assay. I would imagine that the lab will ask for high purity samples of both a- and b- estradiol as refence materials.
You would need to consult with the lab; and maybe a couple of labs for alternate opinions.
and…
Also, 100% is somewhat nebulous. It could mean that the estradiol is 100% a- or b-, but has some other stuff as carrier (water, saline, buffer, other steroids not estradiol, etc).
Or it could mean that the sample is actually 100% estradiol (a- or b-), with no other compounds (no fillers, excess proteins, saline, buffers, etc)
My thoughts are that it is a high % of one diastereomer in a mix that contains many other chemicals including byproducts, buffers, water, etc.
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Thanks for updating the information of 17-Alpha Estradiol, I think there are too few people using 17-Alpha Estradiol right now, according to the survey in this site, only 1% users in this site have experience in 17-Alpha Estradiol.
I wish there are more advice and feedback from people and MD, it looks like 17-Alpha Estradiol will not be available for the next decade, do you know whether there is any company developing 17-Alpha Estradiol as drug? And what’s the estimated time for FDA to approve 17-Alpha Estradiol for prescription Rapamycin User Survey #2 - Please Respond
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Hi All
I have procured a source of 99.5% pure 17alpha estradiol in pharmaceutical cream delivery base provided in a pump bottle of 100mg/50ml with a 2mg/1ml delivery per pump.
We are planning on a small trial for proof of efficacy and safety
Markers to include:
Serum or urine 17a estradiol levels**
Serum Chemistry
GlycanAge Immune Age
TruDiagnostic Pace of Aging
Precision Analytics Comprehensive Urine Hormone Metabolic
CNS Vital Signs
I have everything lined up except for a lab to assess 17alpha estradiol levels. Our best guess for a starting dose would be 8 to 12mg per week. Ideally this could be a twice weekly dose but we may want to go with 1 pump 5 to 6 days weekly. Before starting the trial we would need some PK data to pick
a dosing protocol.
If anyone knows of a lab or can be of help finding a lab, I would greatly appreciate it. I have sent some emails out to researchers of some more recent papers. So hoping I will get a response.
Thoughts? Ideas? Feel free to message me directly at 805.724.6446
Thanks
Rick Cohen, M.D.
.
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I know someone who is working to separate the diasteromers of MDMA (one of them is far less neurotoxic).
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Does anyone know if 17-alpha-estradiol is enough to maintain bone density? (esp in those who want to reduce their testosterone? [yes i know T is necessary for the MOA of 17AE]
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Keep us posted on how it goes
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I wanted to share some interesting bloodwork that came back after a few months of using topical Alfatradiol from Ell-Cranell (hair formula) mixed with ethoxydiglycol (transcutol).
I had no idea whether it was absorbing systemically, but my last blood test freaked out my doctor because my estradiol was elevated at 175 pmol/L (ref <162 for males) and my IGF-1 was 225 (ref 65-200 mcgl/L). I told him about the topical Alfatradiol and he said that the blood test here probably doesn’t distinguish between 17-alpha estradiol and 17-beta estradiol (estrogen). He wasn’t happy with my high IGF-1, but found this paper showing 17-a E upregulates IGF1 production.
Together, this provides some compelling evidence (for me, anyway) that the 17-a E is in fact absorbing topically.
Whether I should worry about the elevated IGF1, I’m less sure. Doc suggested that I go off the hair tonic for a month before the next blood test, just to be sure that’s what’s causing this.
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Have you experienced any changes with weight or muscle mass? I’ve had my IGF up at those levels and I was a larger human
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I don’t think so. I periodize my training and spent Sept through Dec focusing on strength, so I did gain some muscle, but I think it was more deadlifts than 17aE. If you look at the paper I attached, it states, “We demonstrate that 17α-E2 increases hepatic insulin-like growth factor 1 (IGF1) production in male mice without inducing any changes in pulsatile growth hormone (GH) secretion.”
Without the GH, this is not a normal, bodybuilder-style IGF1 increase. Which is why I’m unsure how negative it is. I have a smart doctor, but he’s also unsure.
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The increase in IGF-1 levels is very interesting. I wonder if they saw that at all in the mouse studies with 17-AE? Its either too low to be significant, or the benefits of 17AE were significantly higher than the negatives of increased IGF1. Definitely something we will want to track over time.
The new longevity drug coming out from Loyal is, as you may know, targeted at reducing IGF1 to increase lifespan, see this link for details: The Longevity Summit, News & Update - #9 by RapAdmin
And of course Laron syndrome suggests that higher igf1 isnt helpful for healthy longevity
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Curious - did you use about 3-4 drops of 50% ethanol with a moist tongue and oral mucosa (high concentration can dry your mouth quickly or make a dry mouth burn) or a lot more than I’m thinking?
I’ll also note that the effects of sublingual are pretty quick and the amounts used are low - I suspect a quick effect within a minute or less, perhaps there are some pharmacokinetics studies on sublingual 17bE2.
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Good question to pose to Rich Miller
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3mg 17-alpha estradiol in 15ml ethanol 50% under tongue, extremely irritating, so I don’t use ethanol now, I used EVOO instead.
I have a question, if I put EVOO underneath tongue for 20 mins, is that dangerous? will the oil molecule be directly transferred to circulating system, which cause embolism?
Ah makes sense with 15 mL…very generally speaking, the “research chemical” crowd that can involve a few clandestine chemists taking certain very much illegal substances that are generally harmful at the doses taken do 5-10 drops around 20-50% ethanol depending on solubility and my observations are it appears to work for them very much anecdotally as a very low cost option to preserve whatever expensive chemicals they are using and bypass first-pass liver metabolism. One generally calculates these parameters carefully in that context.
As for EVOO, all I can say is as general information - such a fat embolism deal generally is trauma related to where one actually has laceration and oil-based sublingual mixes are also fairly common.
I’d imagine that if we were designing an experiment in a human trial - just a sublingual solid tablet of 17aE2 could work in theory as well - but do not rely.
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Dr Stanfield is my go to on longevity supplements. On any study he will check the data against the conclusion and at times find that the data does not support the conclusion. And it is the conclusion that makes it into the media supported or not by the data.
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I have a friend who’s making it in capsule dose now (has access to private labs) - what dose would you want it to be in?
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