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Purity: ≥98%
SC-26196 is a novel, potent and orally bioactive D6D (Delta6 desaturase) inhibitor with IC50 of 0.2 µM in a rat liver microsomal assay. It 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.
| ln Vitro |
The proliferation of peripheral blood mononuclear cells (PBMC) is inhibited by SC-26196 (200 nM), but not that of Jurkat cells [2].
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| ln Vivo |
The computed Δ6-desaturase index in adipose tissue and liver decreased with the addition of SC-26196 to the diet (at doses of 0, 0.07, 0.21, or 0.7 mg/kg to obtain dosages of 0, 10, 30, and 100 mg/kg per day). Δ6-desaturase is inhibited when 100 mg of SC-26196 are fed daily per kilogram of body weight [3].
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| Cell Assay |
Cell proliferation assay [2]
Cell Types: PBMC and Jurkat cells Tested Concentrations: 200 nM Incubation Duration: 96 hrs (hours) for PBMC; 144 hrs (hours) for Jurkat cells Experimental Results: PBMC treatment Dramatically diminished the proportion of dividing cells, division index and proliferation index. Cell proliferation of Jurkat cells was not Dramatically altered. |
| Animal Protocol |
Animal/Disease Models: Male mice (12 or 15 weeks old) [3]
Doses: 0, 10, 30 and 100 mg/kg daily Doses: included in the diet at 0, 0.07, 0.21 or 0.7 mg/kg diet to achieve doses of 0, 10, 30 and 100 mg/kg per day. Experimental Results: Caused a decrease in calculated Δ6-desaturase index in adipose tissue and liver. |
| References |
[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. |
| Molecular Formula |
C27H29N5
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| Molecular Weight |
423.55266
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| CAS # |
218136-59-5
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| SMILES |
N#CC(C1=CC=CC=C1)(C2=CC=CC=C2)CCCN3CCN(/N=C/C4=CC=CN=C4)CC3
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~11.80 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3610 mL | 11.8050 mL | 23.6100 mL | |
| 5 mM | 0.4722 mL | 2.3610 mL | 4.7220 mL | |
| 10 mM | 0.2361 mL | 1.1805 mL | 2.3610 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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