Ifetroban
Based on 1 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.65%
- CAS No.: 143443-90-7
- Formule: C25H32N2O5
- Masse moléculaire:440.53
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Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Ifetroban
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Activité biologique
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TXA2/TP |
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.
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Cell Line:Mouse pulmonary microvascular endothelial cells (MPMECs) and human umbilical vein endothelial cells (HUVECs)
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Concentration:100 nM
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Incubation Time:6 hours
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Result:Decreased the level of TPr protein and inhibited PKC substrate phosphorylation.
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Cell Line:Mouse pulmonary microvascular endothelial cells (MPMECs) and human umbilical vein endothelial cells (HUVECs)
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Concentration:100 nM
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Incubation Time:6 hours
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Result:Showed transendothelial migration of GFP+ 4T1 and MDA-MB-231 across mouse MPMECs and human HUVECs.
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.
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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]
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Dosage:50 mg/kg; via 25 μL vehicle (4% sucrose in sterile water)
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Administration:Oral gavage; pretreated before 2 days and treated 28 days later
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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%.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 143443-90-7
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Appearance Solid
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Masse moléculaire 440.53
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Formule C25H32N2O5
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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
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Synonyms
BMS-180291
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
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 |
Ifetroban Related Classifications
HY-105218 Related Classifications
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