Mirodenafil dihydrochloride (Synonyms: SK-3530 dihydrochloride)
目录号: PL09732 纯度: ≥99%
CAS No. :862189-96-6
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中文名称
Mirodenafil dihydrochloride
中文别名
米罗那非二盐酸盐
英文名称
Mirodenafil dihydrochloride
英文别名
Mirodenafil Dihydrochloride;5-Ethyl-2-(5-{[4-(2-hydroxyethyl)-1-piperazinyl]sulfonyl}-2-propo xyphenyl)-7-propyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one d ihydrochloride;Mirodenafil Dihydroc;SK3530 dihydrochloride;SK-3530 dihydrochloride;Mirodenafil dihydrochloride
Cas No.
862189-96-6
分子式
C26H37N5O5S.2[HCl]
分子量
604.59
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
Mirodenafil (SK3530) dihydrochloride 是一种口服有效、可逆的、选择性的磷酸二酯酶 5 (PDE5) 的抑制剂。Mirodenafil dihydrochloride 是一种糖皮质激素受体 (GR) 的调节剂。Mirodenafil dihydrochloride 通过下调 Dkk1 的表达,激活 Wnt/β-catenin 信号通路。Mirodenafil dihydrochloride 可用于研究勃起功能障碍 (ED)、阿尔茨海默病 (AD) 和系统性硬化症 (SSc)。
生物活性
Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
性状
Solid
IC50 & Target[1][2]
PDE5
体外研究(In Vitro)
Mirodenafil dihydrochloride (0-40 μM, 24 h) exerts neuroprotective functions via activating the cGMP/PKG/CREB signaling pathway.
Mirodenafil dihydrochloride (0-40 μM, 24 h) enhances neuronal survival by protecting the mitochondrial membrane potential and inhibiting apoptosis.
Mirodenafil dihydrochloride (0-40 μM) inhibits GSK-3β signaling, resulting in reduced tau phosphorylation, decreased Aβ production by inhibiting amyloidogenesis and activating the autophagosomal pathway.
Mirodenafil dihydrochloride inhibits the transcriptional activity of the glucocorticoid receptor (GR), and inhibits homodimerization of GR in HT-22 cells.
Mirodenafil dihydrochloride (0-100 μM, 24 h) inhibits TGF-β-induced phosphorylation of Smad2/3 and mRNA expression of the fibrosis marker in fibroblasts.
体内研究(In Vivo)
Mirodenafil dihydrochloride (4 mg/kg, IP, daily for 4 weeks) enhances the cognitive-behavioral performance in transgenic AD mice.
Mirodenafil dihydrochloride (0-10 mg/kg, Orally, daily for 3 weeks) ameliorates dermal fibrosis in a BLM-induced SSc mouse model by inhibiting the TGF-β signaling pathway, thereby suppressing the expression of collagen and profibrotic genes. 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, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
ClinicalTrial
参考文献
[1]. Park HJ, et al. Mirodenafil for the treatment of erectile dysfunction: a systematic review of the literature. World J Mens Health. 2014 Apr;32(1):18-27.
[2]. Kang BW, et al. Phosphodiesterase 5 inhibitor mirodenafil ameliorates Alzheimer-like pathology and symptoms by multimodal actions. Alzheimers Res Ther. 2022 Jul 8;14(1):92.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (165.40 mM)H2O : 5 mg/mL (8.27 mM; ultrasonic and warming and heat to 60°C)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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