产品
编 号：F627620
分子式：C20H21N3O5S
分子量：415.46
分子式：C20H21N3O5S
分子量：415.46
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 1090893-12-1
产品详情
生物活性：
Z62954982 (ZINC08010136) is a potent, selective and?cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982?disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).
体内研究：
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.
体外研究：
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 IC50 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 (ZINC08010136) is a potent, selective and?cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982?disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).
体内研究：
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.
体外研究：
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 IC50 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.
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