Sirolimus Powder - 3rd party analysis

[MAC]

Rapamycin here in Canada is prohibitively expensive. Quoted Rapamune, $1000CDN for 100 x 1mg tablets, or $8 USD/mg. So I started to search for alternate sourcing. Thankfully, a fairly robust online community of bio-hackers had paved the way.

When I started Rapamycin back in January 2021, some posters in another forum vouched for a capsulized product out of Austrialia: http://rapamycin.store/ (30 capsules @ 4mg/capsule, approx $1 US/mg delivered). I had ordered/consumed several several batches. For the past 4 weeks, I upped me dose to “18mg” with GFJ per week, no significant side effects.

As the year progressed, I considered alternative sourcing. Some other posters have vouched (3rd party analysis, personal side effects) for Rapamycin sourced from http://www.hhdpharm.cn/en-us/ (WHP)

I was quoted:

USD$60 Per 1000mg
USD$120 Per 2000mg
USD$300 Per 5000mg

+$50 for shipping, and any wire fees (typically $15 USD).

Good service, easy to deal with.

I lost my first 1g shipment to Customs, but ordered a 2nd shipment (I redirected from WHP to a business contact in China, who repackaged, on-forwarded to me) of 4000mg for $220 delivered, or USD, $0.055/mg. They gave me a deal on 2nd order to compensate for the lost shipment.

My contact: hhdpharm06@outlook.com (Sophia Jiang)

Wanting to make certain the powdered sample was indeed Rapamycin and had no other safety concern contaminants, I sent it out to a local 3rd party lab for mass spectrophotometry. I also sent out a 6mg capsule (a custom capsule order) from http://rapamycin.store/

The test cost me $200 CDN per sample (approx $160 USD)

The results of the scan on the WHP sample attached.

Summary

1. The WHP sample is definitely Rapamycin. There are some additional signals indicative of product degradation (per lab). Sirolimus powder, unstabilized (eg a conjugated salt form for stability), must be stored at -20C to prevent degradation. Testing lab confirmed same re storage for Rapamycin powder. My sample, based on the testing, is likely 85-90% Rapamycin, rest is degradation products of Rapamycin (approx 6 weeks out of cold storage from vendor). No signal for any other significant contaminants or unsafe molecules indicated. I have my sample in the home freezer, which should be about -15/-20C.

Rapamycin VETRANAL, analytical standard 53123-88-9

" storage temp. −20°C"

2. The rapamycin.store sample also confirmed Rapamycin (results not posted). Impossible for lab to confirm exact level, but the 6mg claimed +/- is likely indicated. This is re-assuring, I’d been taking this for 15 months. Although, it too, most certainly had degradation. I had NOT been storing these capsules in a deep freezer. Vendor packaging advises to store at room temperature…

So I will proceed with the WHP, and with 4,000 mg, I have plenty to do more in depth trough/peak/side effects testing, although I need to prorate dosing for the less than 100% level.

For those sourcing raw powders overseas, you have to know the sample is most likely not 100% Rapamycin as starters, and may have other contaminants, unless you independently confirm otherwise. And critical for yield, keep in freezer any material prior to taking.

Even adding the $160 USD for independent lab test, and factoring in say 90% Rapamycin, my all-in cost ($220+$160)/(4000x0.9) = $0.105 USD/mg. About a tenth of what I was paying prior, and 80X less than prescription.

I will post any blood Sirolimus level experiments I conduct.

MASS SPECTROPHEMETRY - WHP - SIROLIMUS 04-25-22.pdf (190.9 KB)

[RapAdmin]

Thanks for sharing - great to see more lab analysis results.

I may be overly cautious - but I would still be concerned with possible contaminants that may be there in low doses, but that you haven’t looked for. (here is a longer writeup on my concerns about drug and nutritional supplement powders sourced from China)

Also - will have a friend with a PHD in chemistry to review the mass spec results, and will report back. I’m not knowledgeable enough to know how to read the results you’ve presented.

UPDATE 4/27/2022 1:18pm: Here are my Chemistry PHD / professor friend’s commentary on the above Mass Spec Test of Rapamycin Powder:

There are 3 traces. The top two seem to be samples, and the bottom the Aldrich standard.

Of the 2 samples, the 1st one is mostly something else, while the 2nd is “pretty” good. There is no indication of what the other stuff is without a closer study.

Unfortunately, with rapa, the possible contaminants could be numerous and difficult to determine without an understanding of the product preparation and component history.

I would avoid Sample 1 without knowing what the identity of the large peak at RT 12.28 min.

[MAC]

I have reams of very detailed analysis from the lab, private communication. The phD tech didn’t see anything of concern molecular or signal level.

That is not to say the sample is 100.000% Rapamycin or degradation products thereof.

If one is super risk averse, buy legit pharma.

[EnrQay]

Does anyone know if storage of rapamycin in the freezer is advised? I bought about a year’s worth and I’m currently keeping it at room temperature.

[RapAdmin]

@EnrQay is this tablet or powder rapamycin?

Here is what the Pfizer website says:

Rapamune Oral Solution bottles should be stored protected from light and refrigerated at 2°C to 8°C (36°F to 46°F). Once the bottle is opened, the contents should be used within one month. If necessary, the patient may store the bottles at room temperatures up to 25°C (77°F) for a short period of time (e.g., not more than 15 days for the bottles).

Rapamune Tablets should be stored at 20°C to 25°C [USP Controlled Room Temperature] (68°F to 77°F). Use cartons to protect blister cards and strips from light. Dispense in a tight, light-resistant container as defined in the USP.

Source: RAPAMUNE® How Supplied/Storage and Handling (sirolimus) | Pfizer Medical Information - US

[MAC]

I am not an expert, but I “think” the pharma companies selling tablets, the powder is stabilized, allowing storage at room temperature (very common).

Raw Sirolimus powder (unstabilized) for certain must be stored at -20C.

[MAC]

Raw powder should be stored at -20C, yes, freezer.

At room temperature, it’s degrading.

[RapAdmin]

Is there any source you can post for this information on storage of the sirolimus powder?

[MAC]

Yes, see my SIGMA ALDRICH link original post. The phD reconfirmed this to me.

[RapAdmin]

Ah yes - see it in the rapamycin / sirolimus data sheet:

https://www.sigmaaldrich.com/deepweb/assets/sigmaaldrich/product/documents/289/717/r0395pis.pdf

RAPAMYCIN
Product Number R0395 Storage Temperature –20 °C

[Potionology]

Very interesting ! and I figured that the raw rapamycin despite some risk which is the case with tablets too , does have some advantages… for example no fillers.

Side note I wonder if any suppliers would ship with icepacks or something like that to minimize the degradation during shipment or would that be too over the top lol

[MAC]

I cannot judge this relative risk, but I’d put WAY more stock on pharma grade stuff being 99.999% pure, at minimum, benign trace elements.

[RapAdmin]

@MAC

I’d put WAY more stock on pharma grade stuff being 99.999% pure

Are you talking about the tablets or the powders here?

I searched on the had-harm.cn website you listed above - can’t find sirolimus on it, and the search feature crashes if you try it…

I would see the powder as a good solution for people using rapamycin topically - in hair or skin serums or creams. Its a very cost-effective solution, and for topical /skin applications I’ve seen research that says it doesn’t get into the blood stream, so I’d personally be less concerned about any possible contaminants in the powder.

[MAC]

Sorry, anything legit pharma, powder or tablets.

http://www.hhdpharm.cn/en-us/ and search, yes you are right.

I was only given the contact, had not really gone through their site.

[EnrQay]

@RapAdmin

Rapamune Tablets should be stored at 20°C to 25°C [USP Controlled Room Temperature] (68°F to 77°F).

I have tablets, so it seems as if I ought to keep them cool, say in the fridge, during the hot summer months. Since they advise freezing powder, I assume refrigeration of tablets would be effective and not harmful to them.

[RapAdmin]

I don’t think there would be any issue with keeping them in the fridge (or freezer) if you live in a hotter climate. Especially if they are packed in the moisture-proof bubble pack that we typically see in the India-provided rapamycin:

[Steveroedde]

Thanks so much for posting this MAC. Also for the clarification that what was misinterpreted as readouts from separate samples in the PDF are all of the WHP sample, and that there is no need to fear the “unknown spike”.
I too have far more faith taking my WHP compound than untested pills from elsewhere… I got burned with placebo from a well known supplier… and posted to alert others… which what led me to China…
My uncompounded drug remains in the freezer, and I only keep compounded product on hand for a month or two. Everything else
goes back to the sealed bags in my freezer.

[MAC]

Yes, the PDF posted, all images relate to the WHP sample.

From the mass spec lab:

“The top panel shows an overview of what is ionizing in negative mode, the middle shows the overview of ionization in positive mode, and the bottom panel indicates the presence of the ion corresponding to Rapamycin. I am currently awaiting the results from the un-targeted search for potential contaminants, however, it does look as though there will be some potential degradation products from the Rapamycin in this sample"

[RapAdmin]

Response From my PHD Chemistry friend:

Ok, so rapa is unstable under strong ionizing conditions; not surprising given the molecular complexity.

It would be best to compare the Aldrich sample to the same analyses to confirm that the (+) and (–) traces do not represent contaminants with unknown metabolic effects.

[MAC]

That would be a good additional experiment, agreed. Happy to send you a sample if so inclined.