2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. Atopaxar hydrobromide

Atopaxar hydrobromide  (Synonyms: E5555 hydrobromide; ER 172594-06)

Cat. No.: HY-18200B
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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.

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

Atopaxar hydrobromide Chemical Structure

Atopaxar hydrobromide Chemical Structure

CAS No. : 474550-69-1

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Atopaxar hydrobromide Related Antibodies

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Description

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[1][2].

IC50 & Target

PAR-1[1]
In Vitro

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 Related Antibodies
In Vivo

Atopaxar (30-100 mg/kg; p.o.) hydrobromide causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model[2].
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.

Animal Model: Guinea pigs, PIT model[2]
Dosage: Oral administration
Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg
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.
Clinical Trial
Molecular Weight

608.54

Formula

C29H39BrFN3O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

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

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

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    Atopaxar hydrobromide (E5555) is prepared in the 0.5% methylcellulose solution[2].

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Purity & Documentation
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Atopaxar hydrobromide 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:

Atopaxar474550-69-1E5555 ER 172594-06E 5555E-5555Protease Activated Receptor (PAR)Thrombin receptorsthrombinreceptorprotease-activatedreceptor-1PAR-1atherothromboticplateletssignalingInhibitorinhibitorinhibit

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