Ifetroban (BMS-180291) sodium 是一种具有口服活性的血栓素 A2 (TXA2) 或前列腺素 H2 (PGH2) 受体拮抗剂。Ifetroban sodium 具有抗血小板活性，可抑制肿瘤细胞迁移，但不影响细胞增殖。Ifetroban sodium 可用于心肌缺血、高血压、中风、血栓、心肌病的研究。
| 生物活性 | Ifetroban (BMS-180291) sodium is an orally active antagonist ofthromboxane A2(TXA2) orprostaglandin H2(PGH2) receptor. Ifetroban sodium shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban sodium can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research[1][2][3][4]. |
| IC50& Target | Thromboxane A2 receptor; Prostaglandin H2 receptor[4] |
体外研究
(In Vitro) | Ifetroban sodium (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)[2].
Ifetroban sodium (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)[2].
Western Blot Analysis[2] | Cell Line: | Mouse pulmonary microvascular endothelial cells (MPMECs) and human umbilical vein endothelial cells (HUVECs) | | Concentration: | 100 nM | | Incubation Time: | 6 hours | | Result: | Decreased the level of TPr protein and inhibited PKC substrate phosphorylation. |
Immunofluorescence[2] | Cell Line: | Mouse pulmonary microvascular endothelial cells (MPMECs) and human umbilical vein endothelial cells (HUVECs) | | Concentration: | 100 nM | | Incubation Time: | 6 hours | | Result: | Showed transendothelial migration of GFP+ 4T1 and MDA-MB-231 across mouse MPMECs and human HUVECs. |
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体内研究
(In Vivo) | Ifetroban sodium (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[2].
Ifetroban sodium (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)[2].
Ifetroban sodium (BMS 180,291; 1 and 3 mg/kg, p.o.) inhibits aggregation and antagonizes TP-receptor in monekys. Ifetroban sodium (3 mg/kg, i.v.) causes only marginal and transient hemodynamic effects in anesthetized African green monkeys[3].
| 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[2] | | 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%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 130 mg/mL(281.08 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1621 mL | 10.8106 mL | 21.6212 mL | | 5 mM | 0.4324 mL | 2.1621 mL | 4.3242 mL | | 10 mM | 0.2162 mL | 1.0811 mL | 2.1621 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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