ChemicalBook--->CAS DataBase List--->1006378-90-0

1006378-90-0

1006378-90-0 Structure

1006378-90-0 Structure
IdentificationBack Directory
[Name]

p38 MAPK-IN-1
[CAS]

1006378-90-0
[Synonyms]

CS-2117
p38 MAPK-IN-4
p38 MAPK-IN-1
1,7-Naphthyridine, 4-(2,4-difluorophenyl)-8-(2-methylphenyl)-, 7-oxide
[Molecular Formula]

C21H14F2N2O
[MDL Number]

MFCD28900744
[MOL File]

1006378-90-0.mol
[Molecular Weight]

348.35
Chemical PropertiesBack Directory
[Boiling point ]

527.0±50.0 °C(Predicted)
[density ]

1.27±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 8.33 mg/mL (23.84 mM)
[form ]

Solid
[pka]

0.26±0.40(Predicted)
[color ]

Off-white to yellow
Safety DataBack Directory
[Symbol(GHS) ]

GHS hazard pictograms
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
[HS Code ]

2933998090
Hazard InformationBack Directory
[Uses]

p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
[in vivo]

p38 MAPK-IN-1 (Compound 4; 1 mg/kg for iv and 10 mg/kg for po) has a t1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a Cmax of 5.3 μM for po in male wistar rats[1].
p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg[1].

Animal Model:Male wistar rats[1]
Dosage:10 mg/kg for po and 1 mg/kg for iv (Pharmacokinetic Analysis)
Administration:Po and iv
Result:Had a t1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a Cmax of 5.3 μM for po.
[IC 50]

p38 MAPK: 68 nM (IC50)
[storage]

Store at -20°C
[References]

[1] Lumeras W, et al. 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. J Med Chem. 2011 Nov 24;54(22):7899-910. DOI:10.1021/jm200975u
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