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Updated: Jun 25, 2026

Optimized Analysis of In Vivo and In Vitro Hepatic Steatosis
Published on: March 11, 2017
Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors
Dmitry O Koltun1, Eric Q Parkhill, Natalya I Vasilevich
1Department of Medicinal Chemistry, CV Therapeutics, Inc., Palo Alto, CA 94304, USA. dmitry.koltun@cvt.com
Abstract:
We identified a series of structurally novel SCD (Delta9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modification of the central bicyclic scaffold has proven key to our potency optimization effort. The most potent analog (8g) had IC(50) value of 50 pM in a HEPG2 SCD assay and has been shown to be metabolically stable and selective against Delta5 and Delta6 desaturases.
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