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Novel Small Molecule Agonists of the Relaxin Receptor as Potential Therapy for Heart Failure and Fibrosis

Posted Nov 15 2012 7:00pm

Description of Invention:
The present invention is directed to novel small molecule agonists of the mammalian relaxin family receptor 1 (RXFP1), including human RXFP1. Activation of RXFP1 induces: 1) vasodilation due to up-regulation of the endothelin system; 2) extracellular matrix remodeling; 3) moderation of inflammation by reducing levels of inflammatory cytokines; and 4) angiogenesis. Small molecule agonists of RXFP1 may be useful in treating acute heart failure (AHF), scleroderma, fibrosis, other conditions associated with the biology of relaxin, and in improving reproductive health and wound healing. These compounds are the first and only small molecule agonists of RXFP1.

  • Cardiovascular diseases
  • Ischemia
  • Fibrosis
  • Inflammation
  • Acute heart failure
  • Human and animal reproductive health

  • First and only small molecule agonists of RXFP1
  • Potent and highly selective
  • Bioavailable with excellent exposure
  • Easy to synthesize and scale-up

Development Status:
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)

Juan J Marugan (NCATS)
Wei Zheng (NCATS)
Marc Ferrer-Alegre (NCATS)
Catherine Chen (NCATS)
Alexander Agoulnik (Florida International University)
Noel T Southall (NCATS)
Jingbo Xiao (NCATS)

Patent Status:
HHS, Reference No. E-072-2012/0
US, Application No. 61/642,986 filed 04 May 2012

Relevant Publication:
  1. Chen ZC, et al. Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by utilizing a homogeneous cell-based cAMP assay. J. Biomol. Screen. 2012, accepted.

Collaborative Research Opportunity:
The National Center for Advancing Translational Sciences is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize small molecule agonists of RXFP1. For collaboration opportunities, please contact Krishna (Balki) Balakrishnan, Ph.D. at 301-217-2336 or .

For Licensing Information Please Contact:
Lauren Nguyen-Antczak Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-496-7057
Fax: 301-402-0220

Ref No: 2498

Updated: 11/2012

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