GSK2593074A (Synonyms: GSK'074) |
Katalog-Nr.GC66479 |
GSK2593074A (GSK&7#39;074) ist ein Nekroptose-Inhibitor mit dualer Targeting-FÄhigkeit sowohl auf RIP1 als auch auf RIP3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1337531-06-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK2593074A (GSK'074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3[1].
GSK2593074A (GSK'074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) completely rescues cells from necroptosis under different stimuli in both human and murine cells at IC50~3 nM. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK2593074A inhibits necroptosis with an IC50 of ~3 nM[1].
Cell Viability Assay[1]
Cell Line: | Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929 |
Concentration: | 0.01, 0.1, 1, 10, and 100 nM |
Incubation Time: | 6 hours for MOVAS cells; 3 hours for L929 cells |
Result: | Inhibited MOVAS and L929 cells with the IC50 of 3 nM. |
GSK2593074A (GSK'074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administrated to Apoe-/- mice immediately following pump implantation. Compared to the DMSO group, GSK2593074A-treated mice show significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) as well as a reduced abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A significantly decreases the extent of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05) [1].
Animal Model: | Apoe-/- female mice (9-10 months)[1] |
Dosage: | 0.93 mg/kg/day; 200 µL |
Administration: | Daily i.p. injection; 14 or 28 days |
Result: | Inhibited aneurysm formation in mouse models of aneurysms. |
Cas No. | 1337531-06-2 | SDF | Download SDF |
Überlieferungen | GSK'074 | ||
Formula | C27H23N5OS | M.Wt | 465.57 |
Löslichkeit | DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic) | 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 | 2.1479 mL | 10.7395 mL | 21.479 mL |
5 mM | 0.4296 mL | 2.1479 mL | 4.2958 mL |
10 mM | 0.2148 mL | 1.074 mL | 2.1479 mL |
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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.
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