| CAS NO: | 1221485-83-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 425.42 |
|---|---|
| Formula | C24H21F2NO4 |
| CAS No. | 1221485-83-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 85 mg/mL (199.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 85 mg/mL (199.8 mM) | |
| Solubility (In vivo) | 0.5% methylcellulose: 30 mg/mL |
| Synonyms | Synonym: CBS3830; CBS-3830; CBS 3830; Skepinone-L Chemical Name: 2-[(2,4-difluorophenyl)amino]-7-[(2R)-2,3-dihydroxypropoxy]-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one InChi Key: HXMGCTFLLWPVFM-GOSISDBHSA-N InChi Code: InChI=1S/C24H21F2NO4/c25-16-4-8-23(22(26)10-16)27-17-5-7-20-15(9-17)2-1-14-3-6-19(11-21(14)24(20)30)31-13-18(29)12-28/h3-11,18,27-29H,1-2,12-13H2/t18-/m1/s1 SMILES Code: O=C1C2=CC=C(NC3=CC=C(F)C=C3F)C=C2CCC4=CC=C(OC[C@H](O)CO)C=C14 |
| In Vitro | In vitro activity: Skepinone-L shows concentration-dependent inhibition of HSP27 (Ser82) phosphorylation through the p38 MAPK pathway with a cellular IC50 of approximately 25 nM, and also reduces concentrations of TNF-α, IL-1β and IL-10, regulated by p38 MAPK, with IC50 ranging from 30 to 50 nM. Skepinone-L (1 μM) abrogates the phosphorylation of platelet p38 MAPK substrate Hsp27 activated by stimulation with CRP, thrombin or thromboxane A2 analogue U-46619, and impairs platelet secretion and aggregation. Kinase Assay: Skepinone-L (CBS3830), the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, Skepinone-L (CBS3830) is a valuable probe for chem. biol. research, and it may foster the development of a unique class of kinase inhibitors. |
|---|---|
| In Vivo | In mouse model, oral administration of skepinone-L resulted in very high level of skepinone-L which was 240 nM and higher than the human whole-blood IC50 value of skepinone. Therefore, it resulted in the inhibition of TNF-α by 77% via the inhibition of upstream p38 MAPK. Thus, it demonstrated the pre!eminent pharmacodynamic properties of skepinone-L. |
| Animal model | Mouse |
| Formulation & Dosage | Dissolved in methyl cellulose; 3 mg/kg; p.o. |
| References | Nat Chem Biol. 2011 Dec 25;8(2):141-3; Cell Physiol Biochem. 2013;31(6):914-24. |
m.cnreagent.com