SC-26196 is a D6D inhibitor (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to arachidonic acid (AA). SC-26196 inhibited the desaturation of 2 microM [1-14C] 18:2n-6 by 87-95% in cultured human skin fibroblasts, coronary artery smooth muscle cells, and astrocytes. By contrast, SC-26196 did not affect the conversion of [1-14C]20:3n-6 to 20:4 in the fibroblasts, demonstrating that it is selective for delta6-desaturase.
Chemical Formula: C27H29N5
Exact Mass: 423.2423
Molecular Weight: 423.564
Elemental Analysis: C, 76.56; H, 6.90; N, 16.53
Chemical Name: (E)-2,2-diphenyl-5-(4-((pyridin-3-ylmethylene)amino)piperazin-1-yl)pentanenitrile
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
SC-26196 (200 nM) inhibits proliferation of peripheral blood mononuclear cells (PBMCs), but Not Jurkat Cells.
SC-26196 ( included in the diet at 0, 0.07, 0.21, or 0.7 mg/kg diet to achieve dosages of 0, 10, 30, and 100 mg/kg per day) causes a decrease in the calculated Δ6-desaturase index in both adipose tissue and liver. Feeding 100 mg SC-26196 per kg BW per day inhibits the Δ6-desaturase enzyme.
Wang J, Liang H, Sun M, Zhang L, Xu H, Liu W, Li Y, Zhou Y, Li Y, Li M. Delta-6-desaturase inhibitor enhances radiation therapy in glioblastoma in vitro and in vivo. Cancer Manag Res. 2018 Dec 7;10:6779-6790. doi: 10.2147/CMAR.S185601. PMID: 30584371; PMCID: PMC6289123.
Sibbons CM, Irvine NA, Pérez-Mojica JE, Calder PC, Lillycrop KA, Fielding BA, Burdge GC. Polyunsaturated Fatty Acid Biosynthesis Involving Δ8 Desaturation and Differential DNA Methylation of FADS2 Regulates Proliferation of Human Peripheral Blood Mononuclear Cells. Front Immunol. 2018 Mar 5;9:432. doi: 10.3389/fimmu.2018.00432. PMID: 29556240; PMCID: PMC5844933.
Mulligan CM, Le CH, deMooy AB, Nelson CB, Chicco AJ. Inhibition of delta-6 desaturase reverses cardiolipin remodeling and prevents contractile dysfunction in the aged mouse heart without altering mitochondrial respiratory function. J Gerontol A Biol Sci Med Sci. 2014 Jul;69(7):799-809. doi: 10.1093/gerona/glt209. Epub 2014 Jan 13. PMID: 24418793; PMCID: PMC4111632.
Zhang L, Ramtohul Y, Gagné S, Styhler A, Wang H, Guay J, Huang Z. A multiplexed cell assay in HepG2 cells for the identification of delta-5, delta-6, and delta-9 desaturase and elongase inhibitors. J Biomol Screen. 2010 Feb;15(2):169-76. doi: 10.1177/1087057109356208. Epub 2010 Jan 19. PMID: 20086206.
Hargrave-Barnes KM, Azain MJ, Miner JL. Conjugated linoleic acid-induced fat loss dependence on Delta6-desaturase or cyclooxygenase. Obesity (Silver Spring). 2008 Oct;16(10):2245-52. doi: 10.1038/oby.2008.338. Epub 2008 Jul 24. PMID: 18719641.
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