ARL67156 (FPL 67156) trisodium 是一种ecto-ATPase抑制剂。ARL67156 trisodium 是竞争性 NTPDase1 (CD39)，NTPDase3 和 NPP1 抑制剂，Ki分别为 11，18 和 12 μM。ARL67156 trisodium 可用于钙化性主动脉瓣疾病、哮喘等疾病的研究。
| 生物活性 | ARL67156 (FPL 67156) trisodium is a selectiveecto-ATPaseinhibitor. ARL67156 trisodium is a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, withKis of 11, 18 and 12 μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma[1][2]. |
| IC50& Target | Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1] |
体外研究
(In Vitro) | ARL67156 trisodium (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner[4].
ARL67156 trisodium (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells[5].
ARL67156 trisodium (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes[6].
ARL67156 trisodium (100 μM, 4h) significantly decreases HIV-1replication in macrophages[7].
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体内研究
(In Vivo) | ARL67156 trisodium (1.1 μg/kg/day, administered with osmotic pumps implanted subcutaneously, for 28 days) prevents the development of calcific aortic valve disease in Warfarin (HY-B0687)-treated rats[2].
ARL67156 trisodium (intraperitoneal injection, 2 mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP)[3].
| Animal Model: | Warfarin-induced mineralization rat model[2] | | 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[3] | | 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 25 mg/mL(31.85 mM;Need ultrasonic) DMSO : 1 mg/mL(1.27 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2738 mL | 6.3690 mL | 12.7380 mL | | 5 mM | 0.2548 mL | 1.2738 mL | 2.5476 mL | | 10 mM | 0.1274 mL | 0.6369 mL | 1.2738 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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