MY-5445

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MY-5445  纯度: ≥99.0%

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。

MY-5445

MY-5445 Chemical Structure

CAS No. : 78351-75-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥990 In-stock
5 mg ￥900 In-stock
10 mg ￥1500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect[1][2].

IC50 & Target[1][3]

PDE5

1.3 μM (Ki)

PDE5

6.7 μM (IC50)

PDE4

37 μM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

331.80

Formula

C20H14ClN3
CAS 号

78351-75-4
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Souness JE, et al. Role of selective cyclic GMP phosphodiesterase inhibition in the myorelaxant actions of M&B 22,948, MY-5445, vinpocetine and 1-methyl-3-isobutyl-8-(methylamino)xanthine. Br J Pharmacol. 1989 Nov;98(3):725-34.

    [2]. Chung-Pu Wu, et al. MY-5445, a phosphodiesterase type 5 inhibitor, resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic anticancer drugs. Am J Cancer Res. 2020; 10(1): 164-178.

    [3]. Maud Bollenbach, et al. Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model. Eur J Med Chem. 2019 Sep 1;177:269-290.

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