MY-5445 | PDE5 Inhibitor | AmBeed-信号通路专用抑制剂

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MY-5445 {[allProObj[0].p_purity_real_show]}

货号：A304814

MY-5445 is a specific inhibitor of cyclic GMP phosphodiesterase 5 with IC50 of 0.5 μM.

MY-5445 化学结构
CAS号：78351-75-4

MY-5445 3D分子结构
CAS号：78351-75-4

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MY-5445 纯度/质量文件产品仅供科研

货号：A304814 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell Host Microbe, 2024. Ambeed. [ A163338 ]; • Cancer Res., 2024. Ambeed. [ A295334 ]; • J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]; • J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]; • JBC, 2024, 107935. Ambeed. [ A194396 ]; 更多 >

PDE 亚型比较

产品名称	PDE ↓ ↑	PDE1 ↓ ↑	PDE10A ↓ ↑	PDE2 ↓ ↑	PDE3 ↓ ↑	PDE4 ↓ ↑	PDE5 ↓ ↑	PDE6 ↓ ↑	其他靶点	纯度
Doxofylline	✔									99+%
Deltarasin	+++ PDEδ , Kd: 38 nM									99+%
7-(2,3-Dihydroxypropyl)theophylline	✔									98%
Aminophylline	+ PDE, IC50: 0.12 mM									98+%
Anagrelide HCl	✔									99%+
Irsogladine	✔								AChR,mAChR	98%
PF-8380	+++ Autotaxin, IC50: 2.8 nM									99%+
Dipyridamole	✔									98%
Balipodect			++++ PDE10A, IC50: 0.3 nM							99%+
PF-2545920			++++ PDE10A, IC50: 0.37 nM							97%
Luteolin		+ PDE1, Ki: 15.0 μM		++ PDE2, Ki: 6.4 μM	+ PDE3, Ki: 13.9 μM	+ PDE4, Ki: 11.1 μM	+ PDE5, Ki: 9.5 μM			98%
Milrinone				++ PDE2, IC50: 5.2 μM	++ PDE3, IC50: 2.1 μM				ATPase	98%
Pimobendan					++ PDE3, IC50: 0.32 μM					98%
Cilostazol					++ PDE3, IC50: 0.2 μM					98%
Fenspiride HCl					+ PDE3, pIC50: 3.44	+ PDE4, pIC50: 4.16				98%
(S)-(+)-Rolipram						++ PDE4, IC50: 0.75 μM				98%
Apremilast						+++ PDE4, IC50: 74 nM				98%
GSK256066						++++ PDE4B, IC50: 3.2 pM				98+%
Roflumilast						++++ PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM				99%
Rolipram						+++ PDE4B, IC50: 130 nM				99%+
Cilomilast						+++ LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM				98+%
Avanafil							++++ PDE5, IC50: 1 nM			98%
Vardenafil HCl Trihydrate							++++ PDE5, IC50: 0.7 nM			98%
Tadalafil							++++ PDE5, IC50: 1.8 nM			98%
Icariin							++ PDE5, IC50: 0.432 μM			98%
Sildenafil							✔	+++ PDE6, IC50: 33 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

MY-5445 生物活性

描述

MY-5445 acts as a specific antagonist of cyclic GMP phosphodiesterase, particularly PDE5, exhibiting a Ki value of 1.3 μM. It effectively prevents human platelet aggregation and modulates the ATP-binding cassette transporter ABCG2 selectively, leading to an anti-proliferative effect^[1]^[2]. Additionally, MY-5445 curbs human platelet aggregation by elevating cyclic GMP levels, serving as a valuable tool for investigating the role of cyclic GMP in this process^[1]. MY-5445 selectively counteracts the ABCG2-mediated multidrug resistance in cells with high levels of ABCG2. It enhances the effectiveness of an ABCG2 substrate drug against ABCG2-overexpressing cancer cells resistant to multiple drugs, likely through altering ABCG2's function and/or expression. Additionally, a 48-hour treatment with MY-5445 at a concentration of 3 μM significantly augments apoptosis in S1-M1-80 cells induced by topotecan^[2].

MY-5445 动物研究

Animal study

Administration of MY-5445, ranging from 0.5 to 3 mg/kg via intraperitoneal injection twice daily for a duration of 15 days, significantly alleviates mechanical hypersensitivity^[3].

MY-5445 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.

MY-5445 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.07mL

3.01mL

1.51mL

30.14mL

6.03mL

3.01mL

MY-5445 技术信息

CAS号	78351-75-4
分子式	C₂₀H₁₄ClN₃
分子量	331.798

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(150.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

MY-5445 {[allProObj[0].p_purity_real_show]}

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MY-5445 质控信息

MY-5445 生物活性

MY-5445 动物研究

MY-5445 参考文献

MY-5445 实验方案

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MY-5445 {[allProObj[0].p_purity_real_show]}

MY-5445 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

MY-5445 质控信息

MY-5445 生物活性

MY-5445 动物研究

MY-5445 参考文献

MY-5445 实验方案

MY-5445 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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MY-5445 纯度/质量文件产品仅供科研