Has Anyone Tried Rad-140?

[midlifealpha]

I noticed BlueSky Peptides advertising a new product called RAD-140.

Started to look into it, seems to be a lot of momentum around it but I've yet to see any postings from folks on TRT. Might be a little too new for my taste and it's also quite expensive.

Just wondering if anyone here has done any research.

 

[ERO]

Never heard of it until now, but a quick Google search makes it intriguing for sure. It seems IMHO that a lot of the older SARMS got a lot of hype but they never really worked that well, but some of the newer ones like Rad-140 and LDG-4033 appear to be a lot better on paper at least.

 

[PAUL-E]

It is a SARM and a research chemical. Where ever you get it, it will come from an UnderGround Lab. I wouldnt trust that. Also, there are zero human studies

Defiantly a risk you never really know what your getting sometimes.
lgd-4033 is still moving forward but it's now being called vk5211, I seen on the news some football player was caught with the lgd in his system maybe that's why they changed the name.
MK-677 seems to have a decent amount of data with humans as well.

 

[Vince Carter]

Anything new on this particular SARM with you guys?

 

[MikeXL]

I know that the compounding pharmacy Taylor Made may compound it. They do so with MK 2867 and LGD 4033.

RAD-140 seems to be gaining traction with BBers.

 

[Vince Carter]

I think I only heard about it last nite watching a crossfit video and one of the competitors pissed hot for Testolone and one other banned substance so I googled it and here I am. I make take a 30 day supply with it and see what's up.

 

[MikeXL]

I think I only heard about it last nite watching a crossfit video and one of the competitors pissed hot for Testolone and one other banned substance so I googled it and here I am. I make take a 30 day supply with it and see what's up.

I can tell you all I know, which is not much
- no human trials yet
- pre-clinical studies show its 1/60th as androgenic as testosterone and 40% more anabolic
- based on the above that is a 90:1 anabolic to androgenic ratio
- users report dry gains
- Only observable side effect seems to be anger/irritability in some people
- I dont see much blood work, but may be less harsh on lipids than other SARMs
- Seems to file a void between Ostarineand LGD 4033. Meaning more anabolic than Ostarine but without the water retention of LGD

Check out Greg Doucett on youtube - BBing/PL coach from Canada. He has a vid on it. He really likes it. No affiliation

 

[djpreef]

I think I only heard about it last nite watching a crossfit video and one of the competitors pissed hot for Testolone and one other banned substance so I googled it and here I am. I make take a 30 day supply with it and see what's up.

I'm almost 6 weeks into an 8 week run at 15mg. I would say I don't FEEL different, but I look different. No weight loss, but I'm definitely seeing better either gains or definition. My wife says so too, so it's not just confirmation bias staring back from the mirror. I'll take 6 weeks off when it's done and then I'm going to do it again.

I'm up about three pounds since I started. I have some loose skin from losing 100 pounds a couple of years ago, so it's very hard for me to tell what's going on in the way of a pound or two of fat, but if I have to guess, I'd say it's a split. A little muscle, a little fat. Carnivore diet, been trying to make sure I eat enough to actually support any gains that might come.

 

[swoops36]

I tried a 3 week run of RAD140 at 15-30mg/day along with my usual 200mg/week TRT. I felt great the first week, just mentally always happy and lifts started to go up right away (placebo partly, I’m sure). So I decided to jump from 15mg to 30mg and that’s where problems started. Headaches, fatigue randomly, and I could not stop eating sugar/carbs. Craved them constantly. It reminded me of low e2 symptoms really. So I stopped after 2 weeks of that. It has been 2 weeks off and I’m considering another go at 15mg/day max. I’ve watched a few YouTube videos, but research is scarce for these SARMs

 

[SilverSurfer]

I could not stop eating sugar/carbs. Craved them constantly. It reminded me of low e2 symptoms really. So I stopped after 2 weeks of that. It has been 2 weeks off and I’m considering another go at 15mg/day max. I’ve watched a few YouTube videos, but research is scarce for these SARMs

I’m glad you and another poster mentioned this. I’ve been curious about compounds that help with joint and soft tissue, but I cannot afford to be triggering my dopamine receptors into craving sugars much less my former DOC.

 

[swoops36]

I’m glad you and another poster mentioned this. I’ve been curious about compounds that help with joint and soft tissue, but I cannot afford to be triggering my dopamine receptors into craving sugars much less my former DOC.

I was also looking for something to help alleviate joint issues, but I’m thinking of asking my doc for Deca instead of going with any SARMs.

 

[madman]

Be aware that this paper is based on animals.....not humans!




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



ABSTRACT
This report describes the discovery of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). The characterization of RAD140 in several preclinical models of anabolic androgen action is also described.



Our work in the SARM area resulted in the synthesis and evaluation of a large number of candidate templates. While we found it relatively easy to obtain compounds with high affinity for AR, we struggled to achieve compounds that demonstrated good oral efficacy and high in vivo tolerability. After scanning many potential leads for oral, in vivo activity, we arrived at high affinity compound5 through a combination of synthetic intermediate testing, literature evaluation and fragment combination. We were delighted when 5 demonstrated oral activity in rats.

However, when we performed a pharmacokinetic analysis in rats, we could detect only very low levels of 5 after oral dosing (F < 5%). Further analysis revealed that 5 was efficiently converted to 6 in vivo, presumably by cytochromes P450 in the rat liver. Compound 6 had similar activity to compound 5 in vivo, suggesting that 6 was largely responsible for the activity of compound 5. An in vitro screen with human microsomes revealed rapid metabolism of compound 5, thus indicating this transformation as a potential human metabolic liability and prompting us to prepare compounds in which the 40 -position of the pendant phenyl was blocked from P450-induced hydroxylation. We looked at several analogues containing a 40 -blocking group, and in the course of our efforts we identified compound 7 (RAD140; Figure 1) as our preclinical development candidate.

The synthesis of compound 7 is shown in Scheme 1. We relied on an expeditious, ipso-fluorine substitution of the left-hand side precursor, piece 8, with D-threonine in the presence of K2CO3 in DMSO to give the desired product 9 in workable yields (typically >50%). The D-Thr adduct 9 was coupled with 4-cyanobenzohydrazide under standard coupling conditions using EDCI and HOBt. The resultant product 10 was silylated with TBDMS-Cl, subjected to dehydrative cyclization conditions in the presence of TPP/I2, and then desilyated for the final step. Overall, this has proven to be a reliable and efficient synthesis using a fairly inexpensive, albeit nonproteinogenic amino acid as the chirality source.

The stability of RAD140 was high (t1/2 >2h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats (F = 27-63%) and monkeys (65-75%). 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 (IC50 = 750 nM vs 0.2 nM for progesterone). In vitro functional androgen agonist activity was confirmed in the C2C12 osteoblast differentiation assay, where an EC50 of 0.1 nM was shown (DHT=0.05 nM).




Clinical chemistry indicated the expected lowering of lipids (LDL, HDL, triglycerides). 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.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. We are currently preparing RAD140 for phase I clinical studies in patients suffering from severe weight loss due to cancer cachexia.









Figure1. Structures of testosterone (1), 5R-dihydrotestosterone (2) ,GTxS-22 (3), BMS 562929 (4), initial lead 5, active metabolite 6, and 7 (RAD140).

Scheme 1. Synthesis of Compound 7 (RAD140)

This is the only and the first human study using RAD140 (PHASE I)


Phase 1, First-in-Human Study of RAD140 in Postmenopausal Women With Breast Cancer



Sponsor:
Radius Pharmaceuticals, Inc.

Information provided by (Responsible Party):
Radius Pharmaceuticals, Inc.





Phase 1, First-in-Human Study of RAD140 in Postmenopausal Women With Breast Cancer - Full Text View - ClinicalTrials.gov

It would also most likely have a strong negative effect on lowering of lipids when higher doses are used which many end up doing when cycling SARMS!