SR 8278 |
| Catalog No.GC15275 |
SR 8278은 REV-ERBα 길항제이며 0.47 μM의 EC50으로 REV-ERBα 전사 억제 활성을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1254944-66-5
Sample solution is provided at 25 µL, 10mM.
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REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.[1],[2] SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112.[2] Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.2 SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.[3]
Reference:
[1]. Duez, H., and Staels, B. Rev-erb-α: An integrator of circadian rhythms and metabolism. Journal of Applied Physiology 107(6), 1972-1980 (2009).
[2]. Kojetin, D., Wang, Y., Kameneck, T.M., et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chemical Biology 6(2), 131-134 (2011).
[3]. Vieira, E., Marroquí, L., Figueroa, A.L., et al. Involvement of the clock gene Rev-erb alpha in the regulation of glucagon secretion in pancreatic alpha-cells. PLoS One 8(7), 1-15 (2013).
| Cas No. | 1254944-66-5 | SDF | |
| Chemical Name | (S)-ethyl 2-(5-(methylthio)thiophene-2-carbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate | ||
| Canonical SMILES | O=C([C@H]1N(C(C2=CC=C(SC)S2)=O)CC3=CC=CC=C3C1)OCC | ||
| Formula | C18H19NO3S2 | M.Wt | 361.48 |
| Solubility | ≤15mg/ml in ethanol;≤10mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7664 mL | 13.832 mL | 27.664 mL |
| 5 mM | 0.5533 mL | 2.7664 mL | 5.5328 mL |
| 10 mM | 0.2766 mL | 1.3832 mL | 2.7664 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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