2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Ifetroban

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.

For research use only. We do not sell to patients.

Ifetroban Chemical Structure

Ifetroban Chemical Structure

CAS No. : 143443-90-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Ifetroban:

Ifetroban Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ifetroban

View All Prostaglandin Receptor Isoform Specific Products:

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DP EP FP IP TXA2/TP TXB2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

TXA2/TP

 

In Vitro

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 Related Antibodies

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.
In Vivo

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.

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
Molecular Weight

440.53

Formula

C25H32N2O5
CAS No.
Appearance

Solid

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (227.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2700 mL 11.3500 mL 22.6999 mL
5 mM 0.4540 mL 2.2700 mL 4.5400 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2700 mL 11.3500 mL 22.6999 mL 56.7498 mL
5 mM 0.4540 mL 2.2700 mL 4.5400 mL 11.3500 mL
10 mM 0.2270 mL 1.1350 mL 2.2700 mL 5.6750 mL
15 mM 0.1513 mL 0.7567 mL 1.5133 mL 3.7833 mL
20 mM 0.1135 mL 0.5675 mL 1.1350 mL 2.8375 mL
25 mM 0.0908 mL 0.4540 mL 0.9080 mL 2.2700 mL
30 mM 0.0757 mL 0.3783 mL 0.7567 mL 1.8917 mL
40 mM 0.0567 mL 0.2837 mL 0.5675 mL 1.4187 mL
50 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1350 mL
60 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
80 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7094 mL
100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5675 mL
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Ifetroban Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ifetroban143443-90-7BMS-180291BMS180291BMS 180291Prostaglandin Receptormyocardial ischemiahypertensionstrokethrombosiscardiomyopathyantiplateletmigration inhibitonInhibitorinhibitorinhibit

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