Ifetroban  (Synonyms: BMS-180291)

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^[1][2][3][4].

Thromboxane A2 receptor; Prostaglandin H2 receptor^[4]

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)^[2].
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)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].
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)^[2].
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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

440.53

C₂₅H₃₂N₂O₅

143443-90-7

OC(CCC(C=CC=C1)=C1C[C@@H]2[C@H](C3=NC(C(NCCCCC)=O)=CO3)[C@@H]4O[C@H]2CC4)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Johnson RA, et al. Effect of ifetroban, a thromboxane A2 receptor antagonist, in stroke-prone spontaneously hypertensive rats. Clin Exp Hypertens. 1996 Feb;18(2):171-88.  [Content Brief]

  [2]. Werfel TA, et al. Repurposing of a Thromboxane Receptor Inhibitor Based on a Novel Role in Metastasis Identified by Phenome-Wide Association Study. Mol Cancer Ther. 2020 Dec;19(12):2454-2464.   [Content Brief]

  [3]. Schumacher WA, et al. Antiplatelet activity of the long-acting thromboxane receptor antagonist BMS 180,291 in monkeys. Prostaglandins. 1992 Nov;44(5):389-97.  [Content Brief]

  [4]. Rosenfeld L, et al. Ifetroban sodium: an effective TxA2/PGH2 receptor antagonist. Cardiovasc Drug Rev. 2001 Summer;19(2):97-115.   [Content Brief]