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RAD140 CAS: 1182367-47-0

Category: Inhibitors
Product Name: RAD140
Cat No: I000022
CAS No: 1182367-47-0
Synonyms: RAD-140; RAD 140;
Molecular Formula: C20H16ClN5O2
Molecular Weight: 393.8
SMILES: C[C@H](O)[C@](NC1=C(C)C(Cl)=C(C#N)C=C1)([H])C2=NN=C(C3=CC=C(C#N)C=C3)O2
Solubility: 10 mM in DMSO
Target: androgen receptor (AR)
IC50: 7 nM (Ki, fot androgen receptor)
Storage: Stored at -20°C.
CAS 1182367-47-0,RAD140
  • Description

RAD140(cas 1182367-47-0) is an investigational selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and breast cancer, currently under development by Radius Health, Inc. (RDUS). (source: https://en.wikipedia.org/wiki/RAD140).

in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM).  RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.
in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys.  RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.

  • Spec

Purity≥ 98.0%

  • References

1: Jayaraman A, Christensen A, Moser VA, Vest RS, Miller CP, Hattersley G, Pike CJ. Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Endocrinology. 2014 Apr;155(4):1398-406. doi: 10.1210/en.2013-1725. Epub 2014 Jan 15. PubMed PMID: 24428527; PubMed Central PMCID: PMC3959610.
2: Thevis M, Piper T, Beuck S, Geyer H, Schänzer W. Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105. Rapid Commun Mass Spectrom. 2013 Jun 15;27(11):1173-82. doi: 10.1002/rcm.6558. PubMed PMID: 23650030.
3: Miller CP, Shomali M, Lyttle CR, O'Dea LS, Herendeen H, Gallacher K, Paquin D, Compton DR, Sahoo B, Kerrigan SA, Burge MS, Nickels M, Green JL, Katzenellenbogen JA, Tchesnokov A, Hattersley G. Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Med Chem Lett. 2010 Dec 2;2(2):124-9. doi: 10.1021/ml1002508. eCollection 2011 Feb 10. PubMed PMID: 24900290; PubMed Central PMCID: PMC4018048.

price inquiry for CAS:1182367-47-0, Product:RAD140