Bioactivity | SC-26196 is a potent, orally active Delta6 desaturase (D6D, FADS2) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties[1]. | ||||||||||||
Target | IC50: 0.2 µM (Delta6 desaturase in a rat liver microsomal assay) | ||||||||||||
Invitro | SC-26196 (200 nM) inhibits proliferation of peripheral blood mononuclear cells (PBMCs), but Not Jurkat Cells[2]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
In Vivo | 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[3]. Animal Model: | ||||||||||||
Name | SC-26196 | ||||||||||||
CAS | 218136-59-5 | ||||||||||||
Formula | C27H29N5 | ||||||||||||
Molar Mass | 423.55 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Obukowicz MG, et al. Novel, selective delta6 or delta5 fatty acid desaturase inhibitors as antiinflammatory agents in mice. J Pharmacol Exp Ther. 1998 Oct;287(1):157-66. [2]. Sibbons CM, et al. 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. [3]. Hargrave-Barnes KM, et al. Conjugated linoleic acid-induced fat loss dependence on Delta6-desaturase or cyclooxygenase. Obesity (Silver Spring). 2008 Oct;16(10):2245-52. [4]. Zhang L, et al. A multiplexed cell assay in HepG2 cells for the identification of delta-5, delta-6, and delta-9desaturase and elongase inhibitors. J Biomol Screen. 2010 Feb;15(2):169-76. |