Z62954982
Z62954982 用途与合成方法
Z62954982 (5-100 μM; 4 hours) reduces the intracellular levels of Rac1- GTP in a concentration-dependent manner,and shows the most potent inhibitory action with an IC 50 of 12.2 μM in Human SMCs.Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs.Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers.
Z62954982 (intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks) has no obvious signs of toxicity and decreases both phosphorylation of p38 as well as secreted IL-6 in PASMCs in response to hypoxia in both abr -/- and bcr -/- mice.
| Animal Model: | Male bcr -/- , abr -/- and wt mice (8 to 10-week-old littermates) are exposed to hypoxia (10% O2) or normoxia (21% O2) for 3 weeks |
| Dosage: | 10 mg/kg or 20 mg/kg |
| Administration: | Intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks |
| Result: | Promoted phosphorylation of p38 MAPK and increased IL-6 in Hypoxia in mice. |
