ARL67156 (FPL 67156) triethylamine 是一种ecto-ATPase抑制剂。ARL67156 triethylamine 是竞争性 NTPDase1 (CD39)，NTPDase3 和 NPP1 抑制剂，Ki分别为 11，18 和 12 μM。ARL67156 triethylamine 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) triethylamine is a selectiveecto-ATPaseinhibitor. ARL67156 triethylamine is a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, withKis of 11, 18 and 12 μM, respectively. ARL67156 triethylamine can be used in the research of disease like 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 triethylamine (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner[4].
ARL67156 triethylamine (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells[5].
ARL67156 triethylamine (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes[6].
ARL67156 triethylamine (100 μM, 4h) significantly decreases HIV-1replication in macrophages[7].
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体内研究
(In Vivo) | ARL67156 triethylamine (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 triethylamine (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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| 分子量 | |
| 性状 | |
| Formula | C15H24Br2N5O12P3.(4.3C6H15N) |
| 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: Methanol : 125 mg/mL(108.30 mM;Need ultrasonic) DMSO : 100 mg/mL(86.64 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.8664 mL | 4.3319 mL | 8.6638 mL | | 5 mM | 0.1733 mL | 0.8664 mL | 1.7328 mL | | 10 mM | 0.0866 mL | 0.4332 mL | 0.8664 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。-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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