Na,K-ATPase α4 Inhibitors
Ouabain Derivatives
- User: Male
- Hormonal: Non-Hormonal
-
Delivery type:
- Not Yet Determined
-
Intended Duration:
- Not Yet Determined
- Development Stage: Discovery & Early Development
- Developer(s)/researcher(s): University of Kansas Medical Center, University of Minnesota
Details
- API: Ouabain Derivatives - Multiple Test Compounds
- Target: Na,K-ATPase α4
-
Mechanism of Action:
- Not Yet Determined
- Inactive Materials: Not Yet Determined
- Regimen: Not Yet Determined
- MPT: Not Potential MPT
- Promising Attributes: To be established - concept is in early development
Product Status
Active/Recent Early Development
History
The alpha 4 isoform of Na, K-ATPase has been understood to play a key role in sperm motility since 2000, when its biological functions were isolated and identified by researchers at the University of Cincinnati. This function has continued to be further described and compounds for inhibition of the isoform have been developed by a number of academic centers, most recently by the University of Kansas Medical Center and the University of Minnesota. In 2025, the two universities published the results of inhibitor refinement research, ultimately selecting compound 45, which features a hexahydronaphthalene core and benzyltriazole moiety at C5, as their lead compound for future development as a non-hormonal male contraceptive.
Publications
doi: 10.1074/jbc.M002323200
doi: 10.1177/002215540004800801
doi: 10.1002/mrd.20383
doi: 10.1093/molehr/gal062
doi: 10.1002/mrd.21114
doi: 10.1530/REP-09-0495
doi: 10.1016/j.bbamcr.2011.07.012
doi: 10.2164/jandrol.111.015545
doi: 10.1021/acs.jmedchem.7b00925
doi: 10.1016/j.theriogenology.2020.06.028
doi: 10.1007/s00232-021-00181-2
doi: 10.1093/biolre/ioac052