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

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

目录号: HY-18200
产品使用指南

Atopaxar (E5555) 是一种高效、有口服活性活性的,选择性的,可逆的凝血酶受体蛋白酶激活受体-1 (PAR-1) 拮抗剂。Atopaxar 能干扰血小板信号。Atopaxar 可用于动脉粥样硬化血栓性疾病的研究。

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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.

References
  • 摩尔计算器

  • 稀释计算器

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× = ×
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Keywords:

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

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Atopaxar
目录号:
HY-18200
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