ABR-238901 是一种口服有效的S100A8/A9阻滞剂,可抑制 S100A8/A9 与其受体 RAGE (晚期糖基化终产物受体) 和 TLR4(toll 样受体 4)的相互作用。ABR-238901 具有用于心肌梗塞 (MI) 研究的潜力。
生物活性 | ABR-238901 is an orally active and potentS100A8/A9blocker and inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) andTLR4(toll-like receptor 4). ABR-238901 has the potential for myocardial infarction (MI) research[1][2][3]. |
体内研究 (In Vivo) | ABR-238901 (30 mg/kg/day; gavage; for 3 weeks) causes less angiogenesis and less IL6 and IL10 in MDSCs[1]. ABR-238901 (30 mg/kg/day; gavage) in combination with Bortezomib (0.6 mg/kg; sc; 2 times/week) reduces tumor load compared with treatments of either agent alone[1]. ABR-238901 (30 mg/kg; IP for the first 3 d and thereafter continuously p.o.; daily; for 21 days) leads to gradual deterioration of cardiac function and accelerated left ventricular remodeling in C57BL/6NRJ mice with myocardial ischemia induced by permanent coronary artery ligation. Treatment with ABR-238901 during the first 3 days post-myocardial infarction (MI) restricts the inflammatory damage and promotes a reparatory environment[2].
Animal Model: | C57BL/KaLwRij mice with 5T33MMvv cells[1] | Dosage: | 30 mg/kg | Administration: | Gavage; daily; for 3 weeks | Result: | Caused less angiogenesis.
Caused less IL6 and IL10 in myeloid-derived suppressor cells (MDSCs). |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(84.46 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 2.5340 mL | 12.6701 mL | 25.3402 mL | 5 mM | 0.5068 mL | 2.5340 mL | 5.0680 mL | 10 mM | 0.2534 mL | 1.2670 mL | 2.5340 mL |
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