阿托帕沙
- CAS号:751475-53-3
- 英文名:Atopaxar
- 中文名:阿托帕沙
- CBNumber:CB52521159
- 分子式:C29H38FN3O5
- 分子量:527.63
- MOL File:751475-53-3.mol
- 沸点 :671.0±65.0 °C(Predicted)
- 密度 :1.22
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : 250 mg/mL (473.82 mM; Need ultrasonic)
- 酸度系数(pKa) :7.43±0.20(Predicted)
- 形态 :Solid
- 颜色 :White to off-white
阿托帕沙性质、用途与生产工艺
- 生物活性 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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靶点
PAR-1
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体外研究
Atopaxar inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC 50 of 0.019 μM.
Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner.
Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM.
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体内研究
Atopaxar (30-100 mg/kg; p.o.) causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model.
Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg.
Animal Model: Guinea pigs, PIT model 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.
- 更新日期：2024/11/08
- 产品编号：HY-18200
- 产品名称：Atopaxar
- CAS编号：
- 包装：1 mg
- 价格：685元
- 更新日期：2024/11/08
- 产品编号：HY-18200
- 产品名称：2-(5,6-二乙氧基-7-氟-1,3-二氢-1-亚氨基-2H-异吲哚-2-基)-1-[3-叔丁基-4-甲氧基-5-(4-吗啉基)苯基]乙酮 Atopaxar
- CAS编号：751475-53-3
- 包装：5mg
- 价格：1800元
- 公司名称：Axon Medchem BV
- 联系电话：--
- 电子邮件：info@axonmedchem.com
- 国家：荷兰
- 产品数：477
- 优势度：30
