Molecular Formula | C27H27N5 |
Molar Mass | 421.54 |
Density | 1.256±0.06 g/cm3(Predicted) |
Solubility | Soluble in DMSO (>25 mg/ml) |
Appearance | solid |
Color | Off-white |
pKa | 13.49±0.40(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Use | URMC-099 is an oral bioeffective mixed lineage kinase 3 (MLK3) (IC50=14 nM) inhibitor with excellent blood-brain barrier penetration. |
In vitro study | URMC-099 inhibited LPS-induced TNFα release in microglia and HIV-1 Tat-induced cytokine release in human monocytes. URMC-099 prevents the destruction and phagocytosis of cultured axons by microglia. In vitro experiments, URMC-099 reduced fMLP-induced chemotaxis of wild-type neutrophils. URMC-099 inhibited LPS-induced TNFα release in microglia and HIV-1 Tat-induced cytokine release in human monocytes. URMC-099 prevents the destruction and phagocytosis of cultured axons by microglia. In vitro experiments, URMC-099 reduced fMLP-induced chemotaxis of wild-type neutrophils. |
In vivo study | In mice, URMC-099 showed good pharmacokinetic properties and improved CNS permeability. In vivo, URMC-099 (10 mg/kg I. p.) reduced inflammatory cytokine production, protected neuronal structure, and altered the morphological and ultrastructural response of microglia to HIV-1 Tat exposure. In wild-type mice, URMC099 significantly reduced the entry of neutrophils through fMLP into the peritoneum. In Mice, URMC-099 showed good pharmacokinetic properties and improved CNS permeability. In vivo, URMC-099 (10 mg/kg I. p.) reduced inflammatory cytokine production, protected neuronal structure, and altered the morphological and ultrastructural response of microglia to HIV-1 Tat exposure. In wild-type mice, URMC099 significantly reduced the entry of neutrophils through fMLP into the peritoneum. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.372 ml | 11.861 ml | 23.723 ml |
5 mM | 0.474 ml | 2.372 ml | 4.745 ml |
10 mM | 0.237 ml | 1.186 ml | 2.372 ml |
5 mM | 0.047 ml | 0.237 ml | 0.474 ml |