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编 号:F011331
分子式:C15H21Br2N5Na3O12P3
分子量:785.05
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1mg
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生物活性:
ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma.

体内研究:
ARL67156 trisodium (1.1 μg/kg/天,皮下植入渗透泵给药,持续 28 天) 可防止 Warfarin (HY-B0687) 处理的大鼠发生钙化性主动脉瓣疾病。 ARL67156 trisodium (腹腔注射,2 mg/kg) 可防止 1,6-二磷酸果糖 (FBP) 引起的血清腺苷浓度升高。Animal Model:Warfarin-induced mineralization rat model
Dosage:1.1 μg/kg/day
Administration:Administered with osmotic pumps implanted subcutaneously, for 28 days
Result:Prevented the development of aortic stenosis by lowering the level of apoptosis and mineralization of the aortic valve/aorta.Normalized the level of pAkt (an important kinase involved in the survival pathway).
Animal Model:C57BL/6 mice
Dosage:2?mg/kg
Administration:Intraperitoneal injection, 1 ?h before administration of FBP (100?mg/kg)
Result:Completely abolished the anti-inflammatory effects of FBP (observed by the neutrophil infiltration, hyperalgesia and oedema of the joint).

体外研究:
ARL67156 trisodium (1-100 μM) 以浓度依赖性方式增强神经源性收缩。 ARL67156 trisodium (10 μg/mL,24 h) 增加 ATP 处理的 HMC-1 细胞中 CXCR3 的细胞膜表面的表达 。 ARL67156 trisodium (30 μM,5s) 增强豚鼠心脏突触体中 ATP 促进的去甲肾上腺素释放。 ARL67156 trisodium (100 μM,4h) 显著降低巨噬细胞中的 HIV-1 复制。
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