MY-5445 是一种特异性的 cGMP 磷酸二酯酶PDE5抑制剂,其Ki值为 1.3 μM。MY-5445 能抑制人血小板凝集。MY-5445 是一种ABCG2转运蛋白调节剂,具有抗增殖活性。
生物活性 | MY-5445 is a specific inhibitor of the cyclic GMPphosphodiesterase,phosphodiesterasetype 5 (PDE5), with aKiof 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporterABCG2, with anti-proliferative effect[1][2]. |
IC50& Target[1][3] | PDE5 1.3 μM (Ki) | PDE5 6.7 μM (IC50) | PDE4 37 μM (IC50) |
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体外研究 (In Vitro) | MY-5445 inhibits human platelet aggregation by increasing cyclic GMP content and that it provides a useful probe for elucidating the role of cyclic GMP in platelet aggregation[1]. MY-5445 selectively reverses ABCG2-mediated multidrug resistance in ABCG2-overexpressing cells[2]. MY-5445 reverses ABCG2-mediated multidrug resistance (MDR) by potentiating the cytotoxicity of an ABCG2 substrate drug in ABCG2-overexpressing multidrug-resistant cancer cells, possibly by modulating the function and/or the protein expression of ABCG2[2]. MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis in S1-M1-80 cell[2].
Apoptosis Analysis[2] Cell Line: | Human S1 colon cancer cells, S1-M1-80 cancer cells | Concentration: | 3 μM | Incubation Time: | 48 hours | Result: | Enhanced drug-induced apoptosis in ABCG2-overexpressing cancer cells. |
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体内研究 (In Vivo) | MY-5445 (0.5-3 mg/kg; i.p.; twice a day; for 15 days) produces a significant relief of mechanical hypersensitivity[3].
Animal Model: | C57BL/6J male mice[3] | Dosage: | 0.5 mg/kg, 3 mg/kg | Administration: | Intraperitoneal injection, twice a day, for 15 days | Result: | Alleviated the cuff-induced allodynia. |
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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 : 50 mg/mL(150.69 mM;Need ultrasonic) 配制储备液 1 mM | 3.0139 mL | 15.0693 mL | 30.1386 mL | 5 mM | 0.6028 mL | 3.0139 mL | 6.0277 mL | 10 mM | 0.3014 mL | 1.5069 mL | 3.0139 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%corn oil Solubility: ≥ 2.5 mg/mL (7.53 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.53 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 25.0 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。 |