Sr-9009 and other REV-ERBa agonist

[brofessorx]

I've seen a lot of talk on this and I want to clear this up, so people can stop getting ripped off.

Pharmacological investigations into the biological role of the REV-ERBα have used the sub-optimal chemical probe GSK4112 (1) and, its analogs SR9011 (2) and SR9009 (3)(Figure 1).

10,11

The IV and oral DMPK profiles of compounds 3(SR9009), 4, 10, 16, and 23 were evaluated in a 1 mg/Kg cassette dose experiment in C57Bl/6 mice. Four of the compounds demonstrated essentially identical profiles with short half-lives, high clearance, and low oral bioavailability. Compound 4 (GSK2945) was differentiated from the group with a longer half-life of 2.0 h and an oral bioavailability of 23%,

The remaining four compounds (3(SR9009), 10, 16, 23) would be suitable for acute time-of-day dosing by injectionwhere short exposure of the compound at meaningful levels in desired.

For those that wondered what Jbry did at Olympus an other companies, he spent his free time researching compounds like this!
If you want to research too, here's the link to this study I quoted: Invalid Link Removed
Now you can have fun like Jbry used too! :banana:

 

[Jebrook]

I've seen a lot of talk on this and I want to clear this up, so people can stop getting ripped off.

Thanks for posting.

 

[brofessorx]

Thanks for posting.

And there is lots of promising data on sr9009. It works very well. Rodents don't eat less, do less moving, and loose fat.
But it's injected. At least 2x per day.

 

[brofessorx]

sprotte sent me this pm.

Hi,
Olympus Labs did come out with an SR9009 product and it is available here in EU. So you would say it isn´t acutally SR9009 in their caps? ;-)

I know oral bioavailability is nearly zero, but if you would try it, how much should someone use? 49 mg/day splitted up in 7 portions ;-)?!

cheers,
sprotte

I'll have to look at it. If they don't have things in it to prevent metabolism of it, I'd say it's worthless if it's legit, or spiked with something else
Looked at it. There's nothing on the label to show the bioavailability or half life issues were solved. This is sad.

 

[brofessorx]

Morning bump
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