2. Academic Validation
  3. Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

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.
Chris P Miller 1,  Maysoun Shomali 1,  C Richard Lyttle 1,  Louis St L O'Dea 1,  Hillary Herendeen 1,  Kyla Gallacher 1,  Dottie Paquin 1,  Dennis R Compton 2,  Bishwabhusan Sahoo 2,  Sean A Kerrigan 2,  Matthew S Burge 2,  Michael Nickels 2,  Jennifer L Green 2,  John A Katzenellenbogen 3,  Alexei Tchesnokov 4,  Gary Hattersley 1
Affiliations

Affiliations

  • 1 Radius Health, Inc., 300 Technology Square, Cambridge, Massachusetts 02139, United States.
  • 2 Obiter Research, 2809 Gemini Court, Champaign, Illinois 61822-9647, United States.
  • 3 Department of Chemistry, University of Illinois at Urbana-Champaign, 600 South Mathews Avenue, Urbana, Illinois 61801, United States.
  • 4 Cambridge Major Laboratories, Inc., W130 N10497 Washington Drive, Germantown, Wisconsin 53022, United States.
PMID: 24900290 DOI: 10.1021/ml1002508
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.

Keywords

Androgen; Herschberger assay; SARM; cachexia; oxadiazole; primate.

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