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ELOVL1-27 is an inhibitor of ELOVL fatty acid elongase 1 (ELOVL1; IC50 = 900 nM).1 It reduces lysohexacosanoylphosphatidylcholine (LPC(C26:0)) synthesis in HEK293 cells (IC50 = 13 nM), as well as in primary fibroblasts isolated from patients with cerebral adrenoleukodystrophy (CALD) or adrenomyeloneuropathy (AMN; IC50s = 15-43 nM), neurodegenerative diseases characterized by rapid inflammatory demyelination of the CNS. ELOVL1-27 (2, 16, and 32 mg/kg) reduces blood LPC(C26:0) levels in wild-type mice and rats. It also reduces CNS levels of LPC(C26:0) in an ABCD1-/- mouse model of ALD when administered at a dose of 1 or 10 mg/kg per day for at least three months.
WARNING This product is not for human or veterinary use.
1. Discovery and optimization of pyrazole amides as inhibitors of ELOVL1. J. Med. Chem. 64(24), 17753-17776 (2021).