| CAS NO: | 304896-28-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 434.27 |
|---|---|
| Formula | C23H13Cl2N3O2 |
| CAS No. | 304896-28-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mg/mL (23.0 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | 8% DMSO+30% PEG 300+ddH2O: ~1.5 mg/mL |
| Synonyms | Synonym: AGK-2; AGK-2; AGK-2. Chemical Name: 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide InChi Key: SVENPFFEMUOOGK-SDNWHVSQSA-N InChi Code: InChI=1S/C23H13Cl2N3O2/c24-15-6-8-19(25)18(12-15)22-9-7-16(30-22)11-14(13-26)23(29)28-21-5-1-4-20-17(21)3-2-10-27-20/h1-12H,(H,28,29)/b14-11+ SMILES Code: O=C(NC1=C2C=CC=NC2=CC=C1)/C(C#N)=C/C3=CC=C(C4=CC(Cl)=CC=C4Cl)O3 |
| In Vitro | In vitro activity: In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. AGK2 protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. AGK2 induces both necrosis and caspase-3-dependent apoptosis in C6 glioma cells. SIRT2 also decreases merlin-mutant viability of mouse schwann cells (MSCs) without substantially reducing wild-type MSC viability. Cell Assay: Cells are exposed to different concentrations of AGK2 in 1 mL of 0.3% basal medium agar containing 10% FBS. The cultures are maintained at 37°C in a 5% CO2 incubator for 10-15 days, and the cell colonies are scored using an inverted microscope |
|---|---|
| In Vivo | AGK2 significantly reduces mortality and decreases levels of cytokines in blood (TNF-α: 298.3±24.6 vs 26.8±2.8 pg/mL, p=0.0034; IL-6: 633.4±82.8 vs 232.6±133.0 pg/mL, p=0.0344) and peritoneal fluid (IL-6: 704.8±67.7 vs 391.4±98.5 pg/mL, p=0.033) compare to vehicle control. AGK2 also suppresses the TNF-α and IL-6 production in the culturing splenocytes (TNF-α: 68.1±6.4 vs 23.9±2.8 pg/mL, p=0.0009; IL-6: 73.1±4.2 vs 49.6±3.0 pg/mL; p=0.0051) |
| Animal model | Mice are intraperitoneally given either AGK2 (82 mg/kg) in dimethyl sulfoxide (DMSO) or DMSO alone, and 2 h later subjects to CLP. Survival is monitored for 240 hours. AGK2-treating mice are grouped into (i) DMSO vehicle, and (ii) AGK2, with sham mice (operating but without any treatment) serving as controls. Peritoneal fluid and peripheral blood are examined at 24 and 48 hours for cytokine production |
| Formulation & Dosage | 82 mg/kg; i.p. |
| References | Science. 2007 Jul 27;317(5837):516-9; Oncotarget. 2013 Dec;4(12):2354-65.; Curr Mol Med. 2015;15(7):634-41. |
m.cnreagent.com