Molecular Formula | C21H21ClN2O |
Molar Mass | 352.86 |
Density | 1.179±0.06 g/cm3(Predicted) |
Boling Point | 511.7±45.0 °C(Predicted) |
Solubility | Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml). |
Appearance | White crystalline powder. |
Color | White |
pKa | 1.76±0.50(Predicted) |
Storage Condition | Store at RT |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored under nitrogen or argon at -20° for up to 1 month. |
In vitro study | Median IC 50 values for PK 11195 are 14.2 μM for L. amazonensis , 8.2 μM for L. major , and 3.5 μM for L. braziliensis . The selective index value for L. amazonensis is 13.7, indicating the safety of PK 11195 for future testing in mammals. Time-and dose-dependent reductions in the percentage of infected macrophages, the number of parasites per infected macrophage, and the number of viable intracellular parasites are observed. Electron microscopy reveals some morphological alterations suggestive of autophagy. Interestingly, MCP-1 and superoxide levels are reduced in L. amazonensis -infected macrophages treated with PK 11195 [1] . |
WGK Germany | 3 |
RTECS | NW6987000 |
biological activity | PK 11195 (RP 52028) is a ligand of TSPO, which can target leishmaniasis. its IC50 values for l. amazonensis, l. major and l. braziliensis are 14.2 μ m, 8.2 μ m and 3.5 μ m respectively. |
target | IC50: 14.2 μM ( L. amazonensis ), 8.2 μM ( L. major ), 3.5 μM ( L. braziliensis ) [1] . |
in vitro study | Median IC 50 values for PK 11195 are 14.2 μ m for l. amazonensis , 8.2 μ m for l. major , and 3.5 μ m for l. braziliensis. the selective index value for l. amazonensis is 13.7, indicating the safety of PK 11195 for future testing in mammals. Time-and dose-dependent reductions in the percentage of infected macrophages, the number of parasites per infected macrophage, and the number of viable intracellular parasites are observed. Electron microscopy reveals some morphological alterations suggestive of autophagy. Interestingly, MCP-1 and superoxide levels are reduced in L. amazonensis -infected macrophages treated with PK 11195 [1] . |