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Ifetroban sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ifetroban sodium图片
CAS NO:156715-37-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
BMS-180291 sodium
产品介绍
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.
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%.
Clinical Trial
分子量

462.51

性状

Solid

Formula

C25H31N2NaO5

CAS 号

156715-37-6

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1621 mL10.8106 mL21.6212 mL
5 mM0.4324 mL2.1621 mL4.3242 mL
10 mM0.2162 mL1.0811 mL2.1621 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。