SR 8278CAS# 1254944-66-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1254944-66-5 | SDF | Download SDF |
| PubChem ID | 53393127 | Appearance | Powder |
| Formula | C18H19NO3S2 | M.Wt | 361.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 50 mM in ethanol | ||
| Chemical Name | ethyl 2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1H-isoquinoline-3-carboxylate | ||
| SMILES | CCOC(=O)C1CC2=CC=CC=C2CN1C(=O)C3=CC=C(S3)SC | ||
| Standard InChIKey | UIEBLUZPSFAFOC-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H19NO3S2/c1-3-22-18(21)14-10-12-6-4-5-7-13(12)11-19(14)17(20)15-8-9-16(23-2)24-15/h4-9,14H,3,10-11H2,1-2H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Rev-Erbα antagonist; inhibits Rev-Erbα transcriptional repression (EC50 = 0.47 μM). Blocks activity of Rev-Erbα agonist GSK 4112 in HEK293 cells. Increases expression of glucose-regulating genes, G6Pase and PEPCK in HepG2 cells. |
SR 8278 Dilution Calculator
SR 8278 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7664 mL | 13.832 mL | 27.664 mL | 55.3281 mL | 69.1601 mL |
| 5 mM | 0.5533 mL | 2.7664 mL | 5.5328 mL | 11.0656 mL | 13.832 mL |
| 10 mM | 0.2766 mL | 1.3832 mL | 2.7664 mL | 5.5328 mL | 6.916 mL |
| 50 mM | 0.0553 mL | 0.2766 mL | 0.5533 mL | 1.1066 mL | 1.3832 mL |
| 100 mM | 0.0277 mL | 0.1383 mL | 0.2766 mL | 0.5533 mL | 0.6916 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.[Pubmed:21043485]
ACS Chem Biol. 2011 Feb 18;6(2):131-4.
REV-ERBalpha is a member of the nuclear receptor superfamily that functions as a receptor for the porphoryin heme. REV-ERBalpha suppresses transcription of its target genes in a heme-dependent manner. Recently, the first nonporphyrin synthetic ligand for REV-ERBalpha, GSK4112, was designed, and it mimics the action of heme acting as agonist. Here, we report the identification of the first REV-ERB antagonist, SR8278. SR8278 is structurally similar to the agonist but blocks the ability of the GSK4112 to enhance REV-ERBalpha-dependent repression in a cotransfection assay. Additionally, whereas GSK4112 suppresses the expression of REV-ERBalpha target genes involved in gluconeogenesis, SR8278 stimulates the expression of these genes. Thus, SR8278 represents a unique chemical tool for probing REV-ERB function and may serve as a point for initiation of further optimization to develop REV-ERB antagonists with the ability to explore circadian and metabolic functions.
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