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)