Brand name: Activin type-2B , ACVR2B (ACE-031) is a protein that in humans is encoded by the ACVR2B gene. ACVR2B is an activin type 2 receptor
Generic name: Peptides (Neuromuscular Disease)
Producer / Manufacturer: Canada Peptides
What is Myostatin and Why Stop It?
I have already covered this in detail in my myostatin article. (the word myostatin is red because it is a hyperlink, click on it to learn more about myostatin.)
Simple simple simple version: Myostatin tells muscle cells to not grow and not to replicate. Blocking myostatin will help muscles get bigger, to date there has been only Follistatin that is widely used to block myostatin.
How is it made?
This is how bad people want to stop myostatin, to simply run an experiment this is what they had to do:
1) Take a portion of human DNA that had the genes necessary to code for JUST THE TIP of the myostatin receptor, not the whole thing, just the tip. This was the part that binds to the myostatin protein.
2) Ran a polymerase chain reaction to amplify this gene fragment, but not before they added genetic code so that the digestive enzymes would cut at the precise right location on this synthesized DNA.
3) The new gene, the tip of the myostatin receptor, was attached to a human antibody backbone. Then a bacteria’s DNA was removed in part and this new gene was spliced into the bacteria DNA’s place. This was all packaged in with a genetic signal to amplify our new frankengene’s expression.
4) What we now have is a vector for our new gene. This bacteria will infect the host with the new DNA and the signal for transcription is amplified in the host organism. Like a Trojan Horse which makes its own Greek soldiers, forever. This will produce the actual antibodies that specifically bind to myostatin. This vector was injected into Chinese hamster ovary cells.
Can’t make this stuff up.
5) The genes are expressed and the antibodies are now free in the hamster cells, the hamster serum is then filtered through a column engineered by GE (makers of washers, dryers, blenders and now hamster ovary cell filters) to grab these antibodies out of the hamster cell serum.
6) These purified antibodies are named ACE-031 and injected into male mice at a concentration of 10mg/kg. That means a adult bodybuilder would have to use 1 gram a month. Gold is $42 a gram. ACE-031 is $150,000 a gram. A gram. Cocaine is $100 per gram. Can you imagine the drug trade for this if it catches on? It is literally almost 4,000 times more valuable than gold.
In this study it was determined that the muscle fiber types I and type II were increased in size (Up to a 22% size increase) but not in number, There was no hyperplasia.
ACE-031 out preformed the control at increasing muscle mass
This brings up an interesting question: Myostatin null mice (mice genetically engineered to not make myostatin) had mostly if not all type II fiber growth. With the null mice the result was hyperplasia in addition to the hypertrophy. This was not seen with ACE-031. With ACE-031 there were increases in cell size but NOT number, and both cell types, type I and type II.
What makes it even stranger is ACE-031 has a muscle building effect even in null mice. This means even with no potential for an animal to make ANY myostatin, the ACE-031 works to increase muscle.
This clearly points to the possibility that the ACE-031 blocks more than myostatin and some of what it blocks causes hypertrophy and specifically at the type I fibers. This is likely because the myostatin receptor binds more than just myostatin. Myostatin is specific for its receptor but the receptor is not specific for the myostatin. If you recall from the biochemical gene-geneering section above ACE-031 is made from the receptor head and bound to an antibody. But it is clear it doesn’t just target myostatin, it targets things we don’t know about yet….
To See If This Creepy Nanobot Monster Works, Lets Test It on Overweight Women Who Don’t Lift
In one human study 185 lb women were given 250 mg of this a single time. Why on earth overweight women who don’t lift were the test group or why so much was used is beyond me. Humans tend to require a much lower dose pound for pound than mice. 29 days (not 30, 29) later their muscle mass was 1.1 lb higher, in their thighs! With a price tag of over 150$ a mg this means for $37,000 you can have thicker thighs too! If only the tested group had anything to do with the group who would use ACE-031 we would have evidence of a great muscle builder. I can’t believe they performed such a stupid study. Why test obese women who don’t lift?
This is the only completed human trial as of November 2013. Other companies have not surprisingly also began developing this drug but with different names. With a street dose costing about $40,000 it makes sense this may be a huge cash cow and all the pharm companies want in.
Other drugs underdevelopment to block myostatin: LY2495655 (Lilly), Myo-29 (Wyth), ACE-031 (Acceleron/shire), PF-06252616 (Pfizer), BYM-338 (Novartis), and about 4 others some are targeting follistatin but the point remains.
Activin type-2B , ACVR2B (ACE-031) is a protein that in humans is encoded by the ACVR2B gene. ACVR2B is an activin type 2 receptor. Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. Activins signal through a heteromeric complex of receptor serine kinases which include at least two type I (I and IB) and two type II (II and IIB) receptors. These receptors are all transmembrane proteins, composed of a ligand-binding extracellular domain with cysteine-rich region, a transmembrane domain, and a cytoplasmic domain with predicted serine/threonine specificity. Type I receptors are essential for signaling; and type II receptors are required for binding ligands and for expression of type I receptors. Type I and II receptors form a stable complex after ligand binding, resulting in phosphorylation of type I receptors by type II receptors. Type II receptors are considered to be constitutively active kinases. This gene encodes activin A type IIB receptor, which displays a 3- to 4-fold higher affinity for the ligand than activin A type II receptor.
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