Skepinone-L(CBS3830) - 半岛电竞官方网址

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

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.

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.

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