Enprofylline acts as a selective and competitive A2B receptor antagonist with the K i of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease.
性状
Solid
IC50 & Target[1][2]
A2B receptor 7 μM (Ki)
体外研究(In Vitro)
Enprofylline (300 μM) completely blocks the release of IL-8 by N-ethylcarboxamidoadenosine (NECA). Enprofylline (10 μM) inhibits NECA (10 μM) induced proliferation in a concentration-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
Enprofylline increases heart rate (HR). Injection of Enprofylline (7.5 and 30 mg/kg) increases HR in male WT mouse from 529±23 to 590±20 and 562±20 after the low and high dose, respectively.
A high dose of Enprofylline (30 mg/kg) also decreases temperature compared with saline injection in female (but not in males) WT mice, but a low dose (7.5 mg/kg) has little effect on mouse temperature. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. I Feoktistov, et al. Adenosine A2b receptors evoke interleukin-8 secretion in human mast cells. An enprofylline-sensitive mechanism with implications for asthma. J Clin Invest. 1995 Oct;96(4):1979-86.[2]. M B Grant, et al. Proliferation, migration, and ERK activation in human retinal endothelial cells through A(2B) adenosine receptor stimulation. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2068-73.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (321.85 mM; Need ultrasonic)配制储备液