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编 号:F162593
分子式:C25H32N2O5
分子量:440.53
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生物活性:
Ifetroban (BMS-180291) is an orally active antagonist of thromboxane A2 (TXA2) or prostaglandin H2 (PGH2) receptor. Ifetroban shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research.

体内研究:
Ifetroban (50 mg/kg/d; p.o.; 2 d prior to, through 28 d after tumor injection) decreases hematogenous metastasis of multiple cancer types without in mice model.Ifetroban (50 mg/kg/d; p.o.; 12 d) does not affect primary tumor growth but decreases tumor vessels in mice with 4T1 (mouse mammary cancer).Ifetroban (BMS 180,291; 1 and 3 mg/kg, p.o.) inhibits aggregation and antagonizes TP-receptor in monekys. Ifetroban (3 mg/kg, i.v.) causes only marginal and transient hemodynamic effects in anesthetized African green monkeys.Animal Model:Athymic (nu/nu) Balb/C female mice injected with tumor cells: 4T1 (mouse mammary cancer), MDA-MB-231 (human breast cancer), MiaPaCa2 (human pancreatic cancer), and A549 (human lung cancer) model
Dosage:50 mg/kg; via 25 μL vehicle (4% sucrose in sterile water)
Administration:Oral gavage; pretreated before 2 days and treated 28 days later
Result:Decreased the percentage of mice harboring MDA-MB-231 lung metastases from 90% to 20%, and mice with A549 lung metastases from 60% to 10%.

体外研究:
Ifetroban (CPI211) (100 nM; 48 h) results Tpr inhibition and potently blocks spontaneous metastasis from primary tumors, without affecting tumor cell proliferation, motility, or tumor growth in 4T1 cells (mouse mammary cancer).Ifetroban (100 nM; 6 h) strongly inhibits PKC substrate phosphorylation, and blocks agonist (U46619, HY-108566)-induced TPr diminution in human umbilical vein endothelial cells (HUVECs).
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