Atopaxar hydrobromide
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease.
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- CAS No.: 474550-69-1
- Formule: C29H39BrFN3O5
- Masse moléculaire:608.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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Help & FAQs
Activité biologique
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PAR1 5.1 nM (IC50) |
Atopaxar hydrobromide (0.0001-10 μM; 1h) inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC50 of 0.019 μM[2].
Atopaxar hydrobromide shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC50s of 0.064 and 0.031 μM, respectively, but has no effect on platelet aggregation induced by either ADP or collagen[2].
Atopaxar hydrobromide shows potent and selective inhibitory effects on guinea pig platelet aggregation induced by thrombin and TRAP with IC50s of 0.13 and 0.097 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Atopaxar hydrobromide does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs, PIT model[2]
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Dosage:Oral administration
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Administration:10 mg/kg, 30 mg/kg, 100 mg/kg
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Result:Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls.
Chemical Information
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CAS No. 474550-69-1
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Masse moléculaire 608.54
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Formule C29H39BrFN3O5
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SMILES
COC1=C(N2CCOCC2)C=C(C(CN(CC3=C4C(F)=C(OCC)C(OCC)=C3)C4=N)=O)C=C1C(C)(C)C.[H]Br
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Synonyms
E5555 hydrobromide; ER 172594-06
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
Références
[1]. Chris Dockendorff, et al. Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett. 2012 Mar 8; 3(3): 232–237. [Content Brief]
[2]. Motoji Kogushi, et al. The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs. Eur J Pharmacol. 2011 Apr 25;657(1-3):131-7. [Content Brief]
[3]. Sun J, et al., Discovery and evaluation of Atopaxar hydrobromide, a novel JAK1 and JAK2 inhibitor, selectively induces apoptosis of cancer cells with constitutively activated STAT3. Invest New Drugs. 2020 Aug;38(4):1003-1011. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Atopaxar hydrobromide Related Classifications
HY-18200B Related Classifications
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