Enprofylline 是一种选择性和竞争性的A2B受体拮抗剂，Ki为 7 μM。Enprofylline 还是一种磷酸二酯酶 (phosphodiesterase) 抑制剂。Enprofylline 可用于哮喘、慢性阻塞性肺疾病的研究
| 生物活性 | Enprofylline acts as a selective and competitiveA2B receptorantagonist with theKiof 7 μM. Enprofylline also acts as aphosphodiesteraseinhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3]. |
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体外研究
(In Vitro) | Enprofylline (300 μM) completely blocks the release of IL-8 by N-ethylcarboxamidoadenosine (NECA)[1].
Enprofylline (10 μM) inhibits NECA (10 μM) induced proliferation in a concentration-dependent manner[2].
Cell Proliferation Assay[2] | Cell Line: | Human retinal endothelial cells (HRECs) | | Concentration: | 10 μM | | Incubation Time: | 24, 48, 72 hours | | Result: | NECA (10 μM) induced a time-dependent increase in HREC proliferation as measured by cell counts, achieving approximately 80% of the density of cells exposed to normal growth medium for 3 days.
Enprofylline (10 μM) completely blocked the proliferative effect of NECA when added concurrently with the analogue. |
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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[3].
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[3].
| Animal Model: | A1RKO mice (were cross-bred to C57BL/6 mice for six generations) and A2ARKO mice (were backcrossed to C57BL/6 mice for more than 10 generations)[3] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneally injected (bolus) at 2-h intervals | | Result: | Increased HR in male WT mouse from 529±23 to 590±20 and 562±20 after the low (7.5 mg/kg) and high dose (30 mg/kg), respectively. |
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| 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) |
| 溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(321.85 mM;Need ultrasonic) 配制储备液 | 1 mM | 5.1496 mL | 25.7480 mL | 51.4960 mL | | 5 mM | 1.0299 mL | 5.1496 mL | 10.2992 mL | | 10 mM | 0.5150 mL | 2.5748 mL | 5.1496 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 (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (10.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (10.71 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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