SR9009 a possible future option for treatment of atherosclerosis

[PAUL-E]

Abstract
The nuclear receptors for heme, REV-ERBα and REV-ERBβ, play important roles in the regulation of metabolism and inflammation. Recently it was demonstrated that reduced REV-ERBα expression in hematopoetic cells in LDL receptor null mice led to increased atherosclerosis. We sought to determine if synthetic REV-ERB agonists that we have developed might have the ability to suppress atherosclerosis in this model. A previously characterized synthetic REV-ERB agonist, SR9009, was used to determine if activation of REV-ERB activity would affect atherosclerosis in LDL receptor deficient mice.
Atherosclerotic plaque size was significantly reduced (p < 0.05) in mice administered SR9009 (100 mg/kg) for seven weeks compared to control mice (n = 10 per group).
SR9009 treatment of bone marrow-derived mouse macrophages (BMDM) reduced the polarization of BMDMs to proinflammatory M1 macrophage while increasing the polarization of BMDMs to anti-inflammatory M2 macrophages. Our results suggest that pharmacological targeting of REV-ERBs
may be a viable therapeutic option for treatment of atherosclerosis.
http://www.ncbi.nlm.nih.gov/pubmed/25800870

 

[maxadvance]

Atherosclerotic plaque size was significantly reduced (p < 0.05) in mice administered SR9009 (100 mg/kg) for seven weeks compared to control mice (n = 10 per group).

Sounds like a lot to take. I've taken several 10mg doses in a day, and the stuff is intense to say the least.

 

[PAUL-E]

Atherosclerotic plaque size was significantly reduced (p < 0.05) in mice administered SR9009 (100 mg/kg) for seven weeks compared to control mice (n = 10 per group).

Sounds like a lot to take. I've taken several 10mg doses in a day, and the stuff is intense to say the least.

I've read it has a short half life(less than 30 min) so it was most likely a 100mg injection.
I would think lower more frequent doses threw out the day would be more efficient given the short half life.
I also read it had poor oral bioavailability something like 2-3%

 

[maxadvance]

I've read it has a short half life(less than 30 min) so it was most likely a 100mg injection.
I would think lower more frequent doses threw out the day would be more efficient given the short half life.
I also read it had poor oral bioavailability something like 2-3%

half life is a few hours, I took 10mg in liquid suspension 3 times a day. In pill form oral bioavailability is like zero you're correct. But a few companies have been able to attach it to something and suspend it in alcohol. It is then absorbed under tongue and goes into your bloodstream instead of a pass thru the digestive sytem. The effects are intense and very noticeable. Used to increase endurance.

 

[PAUL-E]

half life is a few hours, I took 10mg in liquid suspension 3 times a day. In pill form oral bioavailability is like zero you're correct. But a few companies have been able to attach it to something and suspend it in alcohol. It is then absorbed under tongue and goes into your bloodstream instead of a pass thru the digestive sytem. The effects are intense and very noticeable. Used to increase endurance.

What did you notice benefits and side effects?