RAD-140

[johnjuanb1]

New SARM - RAD-140​

RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM)

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

RAD140 has all the hallmarks of a SARM. It is potency selective, since it stimulates muscle weight increases at a lower dose than that required increases in body weight over such a short time, there was no elevation of liver enzyme transaminase levels in any animal at any dose >2 fold over its baseline value. Given the well-established relationship between oral androgen use and liver stress indicators, we were quite pleased that at a dose 10-fold greater than the fully effective dose we saw minimal liver enzyme elevations. Taken in sum, RAD140 has all the hallmarks of a SARM. It is potency selective, since it stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases. Moreover, it is also efficacy selective, because it is fully anabolic on muscle but demonstrates less than complete efficacy on the prostate and seminal vesicles and, in fact, can partially antagonize the stimulation of the seminal vesicles induced by testosterone. RAD140 has excellent pharmacokinetics and is a potent anabolic in nonhuman primates as well. We believe the overall preclinical profile of RAD140 is very good, and the compound has completed preclinical toxicology in both rats and monkeys.

Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. - PubMed - NCBI

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. - PubMed - NCBI

Selective Androgen Receptor Modulator RAD140 Is Neuroprotective in Cultured Neurons and Kainate-Lesioned Male Rats

 

[Capin]

Dangit JJ I haven't even opened my yk bottle yet!

 

[johnjuanb1]

Dangit JJ I haven't even opened my yk bottle yet!

Haha the studies show RAD-140 to be dosed at .1mg/kg in monkeys so that's 10mg per day. The higher the dosing the greater the lean muscle tissue.
But even at outrageous mega doses there was virtually no prostate growth or liver toxicity. It works off the androgen receptor and is a partial agonist, I believe, to the progesterone receptor.
I looks like it enhances testosterone propionate. It doesn't compete with it.
I need to read the studies more closely. A SARM that can add to AAS benefits is perfect for me because I never cycle off.
I asked the boss at superior to send samples out for RamboStallone, Elvia, and I, to guinney pig it. I love new toys to play with.

 

[johnjuanb1]

Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats.
Jayaraman A, et al. Endocrinology. 2014.

Abstract
The decline in testosterone levels in men during normal aging increases risks of dysfunction and disease in androgen-responsive tissues, including brain. The use of testosterone therapy has the potential to increase the risks for developing prostate cancer and or accelerating its progression. To overcome this limitation, novel compounds termed "selective androgen receptor modulators" (SARMs) have been developed that lack significant androgen action in prostate but exert agonist effects in select androgen-responsive tissues. The efficacy of SARMs in brain is largely unknown. In this study, we investigate the SARM RAD140 in cultured rat neurons and male rat brain for its ability to provide neuroprotection, an important neural action of endogenous androgens that is relevant to neural health and resilience to neurodegenerative diseases. In cultured hippocampal neurons, RAD140 was as effective as testosterone in reducing cell death induced by apoptotic insults. Mechanistically, RAD140 neuroprotection was dependent upon MAPK signaling, as evidenced by elevation of ERK phosphorylation and inhibition of protection by the MAPK kinase inhibitor U0126. Importantly, RAD140 was also neuroprotective in vivo using the rat kainate lesion model. In experiments with gonadectomized, adult male rats, RAD140 was shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate. These novel findings demonstrate initial preclinical efficacy of a SARM in neuroprotective actions relevant to Alzheimer's disease and related neurodegenerative diseases.

 

[johnjuanb1]

I paraphrased this study.

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

The stability of RAD140 was high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats (F = 27−63%) and monkeys (65−75%). (This shows high oral bioavailability in primates.)

RAD140 demonstrated excellent affinity for the androgen receptor (Ki = 7 nM vs 29 nM for testosterone and 10 nM for DHT) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor

RAD140 increased the weight of the levator ani muscle above that of the intact control starting with the lowest tested dose (0.1mg/kg). (RAD140 builds muscle at dosing of 10mg in a 220Lb "animal")

Interestingly, RAD140 demonstrated no stimulation of the prostate above the intact animal control level until the highest dose tested, 30 mg/kg.
At 0.3 mg/kg, RAD140 demonstrated muscle efficacy similar to Testosterone Propionate at 0.5 mg/kg. (I interpret this to mean 30mg RAD140 per day builds muscle as effectively as 50mg Testosterone Propionate per day in a 220Lb "animal")

MONKEY DOSING INFO

The results on animal body weight of 28-day dosing with RAD140 at 0.01 mg/kg.
In this study, a mean weight gain of greater than 10% in just 28 days of dosing was achieved at a dose of just 0.1 mg/kg ( These monkeys gained 10% muscle in 28 days with the equivalent dose of 10mg per day in a 220Lbs "monkey". That means if you weigh 220Lbs, you would gain 22Lbs of lean muscle in 28 days at 10mg/day, if you respond like a monkey!)
Muscle showed a qualitative trend that increases with dose. Although it appears that the majority of mass increase was due to lean mass increase.
Despite the rather dramatic increases in body weight over such a short time, there was no elevation of liver enzyme transaminase levels in any animal at any dose >2 fold over its baseline value. Given the well-established relationship between oral androgen use and liver stress indicators, we were quite pleased that at a dose 10-fold greater than the fully effective dose we saw minimal liver enzyme elevations.

RAD140 is potency selective, since it stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases. Moreover, it is also efficacy selective, because it is fully anabolic on muscle but demonstrates less than complete efficacy on the prostate and seminal vesicles and, in fact, can partially antagonize the stimulation of the seminal vesicles induced by testosterone. (Taking RAD140 simultaneously with testosterone can lower some negative side effects from testosterone)
RAD140 has excellent pharmacokinetics and is a potent anabolic in nonhuman primates as well.

 

[Massive G]

I have read about RAD for a few months now, but not many sponsors carry it, that I know of.

 

[Bionic]

Haha the studies show RAD-140 to be dosed at .1mg/kg in monkeys so that's 10mg per day.

I don't think that's right.

If what you stated as the effective dosage for monkeys is in fact .1mg/kg, according to this formula, the Human Equivalent Dosing (HED) would be ~3mgs for a 220lbs man.

HED= .1 x 12 / 37
HED= .03mgs/kg

220lbs human = 100kg

.03 x 100 = 3mgs per day.

 

[johnjuanb1]

I don't think that's right.

If what you stated as the effective dosage for monkeys is in fact .1mg/kg, according to this formula, the Human Equivalent Dosing (HED) would be ~3mgs for a 220lbs man.

HED= .1 x 12 / 37
HED= .03mgs/kg

220lbs human = 100kg

.03 x 100 = 3mgs per day.

In your calculation you used the number 12. I think that's the number for baboons. In monkeys the number is 3. Am I off on this?
I'm glad you posted this. I never remember how human dosing compares to the various animals. So we only need 3mg per day?
The studies on rats showed the higher the dose of RAD140, the more muscle gain in the muscle they studied.

 

[Bionic]

I'm glad you posted this. I never remember how human dosing compares to the various animals. So we only need 3mg per day?
The studies on rats showed the higher the dose of RAD140, the more muscle gain in the muscle they studied.

Yes. 3mgs if you're 220 was the lowest effective dose. HED of 9mgs was the dosage (for a 220lbs man) that they say equalled 50mgs per day of Test prop.

One of the things that I did notice was that they used 30mgs/kg and that is where they noticed that it affected the prostate. Hold onto your ass for this one.... The HED would be 972mgs per day for a 220lbs man! LMAO! But please keep in mind that these dosages were studied on NON-HUMAN PRIMATES.

There's no guarantee that Human Primates will experience the same rate of growth/lack of side effects at dosages adjusted accordingly. Would be nice, though.

 

[Bionic]

In your calculation you used the number 12. I think that's the number for baboons. In monkeys the number is 3. Am I off on this?
I'm glad you posted this. I never remember how human dosing compares to the various animals. So we only need 3mg per day?
The studies on rats showed the higher the dose of RAD140, the more muscle gain in the muscle they studied.

Baboons have a Km factor of 20. Refer to the formula atop the table.

 

[johnjuanb1]

Yes. 3mgs if you're 220 was the lowest effective dose. HED of 9mgs was the dosage (for a 220lbs man) that they say equalled 50mgs per day of Test prop.

One of the things that I did notice was that they used 30mgs/kg and that is where they noticed that it affected the prostate. Hold onto your ass for this one.... The HED would be 972mgs per day for a 220lbs man! LMAO! But please keep in mind that these dosages were studied on NON-HUMAN PRIMATES.

There's no guarantee that Human Primates will experience the same rate of growth/lack of side effects at dosages adjusted accordingly. Would be nice, though.

Awesome! Thank you! I'm going to start at 10mg and see what happens. I'm actually on 50mg test prop per day currently, along with a host of other things.

 

[bigbumpkin2003]

Sounds very promising!

 

[johnjuanb1]

NEURON PROTECTION OF RAD140

Selective Androgen Receptor Modulator RAD140 Is Neuroprotective in Cultured Neurons and Kainate-Lesioned Male Rats

In cultured hippocampal neurons, RAD140 was as effective as testosterone in reducing cell death induced by apoptotic insults.

 

[Elvia1023]

Bionic thanks for all the info. I want to start this badly. I mentioned in another thread we get new products in from time to time and I am never excited. You will see in my posts I chat about the same things... tried and tested. I love experimenting though and this sounds like it would be great. Time to turn this monkey into a gorilla

 

[silverTT]

Has the Rad140 been shown to possess hypogonadic aspects as some have said they have noticed with the use of other SARMS like Ostarine?

I would be interested in possibly adding this into a MK cycle however not looking to do so if the expense is at the affect of the HPTA.

 

[Elvia1023]

Hopefully I can start this in the next few weeks to see if it is as good as it sounds. From what I have heard it is very popular so lots of guys should start posting more about it in the next few weeks.

 

[johnjuanb1]

Has the Rad140 been shown to possess hypogonadic aspects as some have said they have noticed with the use of other SARMS like Ostarine?

I would be interested in possibly adding this into a MK cycle however not looking to do so if the expense is at the affect of the HPTA.

I can't find any studies showing HPTA suppression from RAD140. It appears to be incredibly anabolic with no shown negative androgenic sides.

 

[silverTT]

Thanks jj.. Sounds very promising.. It's been several yrs since studying and researching the sarms when they first came out and my biggest concern has been possible suppression with use.. Because if they tend to possess any level of suppression then I would just go ahead and do a test cycle..
But another concern is whether any type of PCT from whatever means may possibly be warranted after utilizing one of the sarms..

 

[Elvia1023]

Thanks jj.. Sounds very promising.. It's been several yrs since studying and researching the sarms when they first came out and my biggest concern has been possible suppression with use.. Because if they tend to possess any level of suppression then I would just go ahead and do a test cycle..
But another concern is whether any type of PCT from whatever means may possibly be warranted after utilizing one of the sarms..

Do what I am going to do and run it with test (and another 15 things)

 

[silverTT]

Haha elvia I'd like to run it with some test along with 15 other things as well! But I've never used more than 2 compounds at once and aside from some low dose var cycles over the yrs it's been probably 15yrs since any legitimate AAS cycle.. I always got extremely good results from very little but tend to shy away from most due to overly sensitive sexual dysfunction with most use..