1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)
  3. Atopaxar

Atopaxar (Synonyms: E5555; ER-172594-00)

Cat. No.: HY-18200
Handling Instructions

Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.

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

Atopaxar Chemical Structure

Atopaxar Chemical Structure

CAS No. : 751475-53-3

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Description

Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2].

IC50 & Target

PAR-1[1]

In Vitro

Atopaxar 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 inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner[2].
Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM[2].

In Vivo

Atopaxar (30-100 mg/kg; p.o.) prolongs the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls[2].
Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2].

Animal Model: Guinea pigs, photo-chemically-induced thrombosis (PIT) model[2]
Dosage: Oral administration
Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg
Result: At 30 and 100 mg/kg prolonged the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls.
Molecular Weight

527.63

Formula

C₂₉H₃₈FN₃O₅

CAS No.

751475-53-3

SMILES

COC1=C(N2CCOCC2)C=C(C(CN(CC3=C4C(F)=C(OCC)C(OCC)=C3)C4=N)=O)C=C1C(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

AtopaxarE5555ER-172594-00E 5555E-5555Protease-Activated Receptor (PAR)Thrombin receptorsthrombinreceptorprotease-activatedreceptor-1PAR-1atherothromboticplateletssignalingInhibitorinhibitorinhibit

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