| 产品描述: | SC-26196 is a potent, orally active Delta6 desaturase (D6D, FADS2) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties |
| 靶点: |
IC50: 0.2 µM (Delta6 desaturase in a rat liver microsomal assay) |
| 体外研究: |
SC-26196 (200?nM) inhibits proliferation of peripheral blood mononuclear cells (PBMCs), but Not Jurkat Cells. Cell Proliferation Assay Cell Line: PBMCs and Jurkat cells Concentration: 200 nM Incubation Time: 96 hours for PBMCs; 144 hours for Jurkat cells Result: Treatment of PBMCs significantly decreased the proportion of cells that underwent division, the division index and proliferation index.Did not alter cell proliferation significantly in Jurkat cells. |
| 体内研究: |
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. Animal Model: Male mice (12- or 15-week-old) Dosage: 0, 10, 30, and 100 mg/kg per day Administration: Included in the diet at 0, 0.07, 0.21, or 0.7mg/kg diet to achieve dosages of 0, 10, 30, and 100mg/kg per day. Result: Caused a decrease in the calculated Δ6-desaturase index in both adipose tissue and liver. |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.361 ml |
11.805 ml |
23.61 ml |
| 5 mM |
0.472 ml |
2.361 ml |
4.722 ml |
| 10 mM |
0.236 ml |
1.18 ml |
2.361 ml |
| 50 mM |
0.047 ml |
0.236 ml |
0.472 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |