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Mirodenafil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mirodenafil图片
CAS NO:862189-95-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
米罗那非
SK3530
产品介绍
Mirodenafil (SK3530) 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 是一种糖皮质激素受体 (GR) 的调节剂。Mirodenafil 通过下调 Dkk1 的表达,激活Wnt/β-catenin信号通路。Mirodenafil 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) is an orally active, potent, reversible, and selectivephosphodiesterase5 (PDE5)inhibitor. Mirodenafil is aglucocorticoid receptor(GR)modulator Mirodenafil activates theWnt/β-cateninsignaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc)[1][2][3].

IC50& Target

PDE5

 

体外研究
(In Vitro)

Mirodenafil (0-40 μM, 24 h) exerts neuroprotective functions via activating the cGMP/PKG/CREB signaling pathway[2].
Mirodenafil (0-40 μM, 24 h) enhances neuronal survival by protecting the mitochondrial membrane potential and inhibiting apoptosis[2].
Mirodenafil (0-40 μM) inhibits GSK-3β signaling, resulting in reduced tau phosphorylation, decreased Aβ production by inhibiting amyloidogenesis and activating the autophagosomal pathway[2].
Mirodenafil inhibits the transcriptional activity of the glucocorticoid receptor (GR), and inhibits homodimerization of GR in HT-22 cells[2].
Mirodenafil (0-100 μM, 24 h) inhibits TGF-β-induced phosphorylation of Smad2/3 and mRNA expression of the fibrosis marker in fibroblasts[3].

Western Blot Analysis[2]

Cell Line:SH-SY5Y human neuroblastoma cells
Concentration:0, 10, 20, 40 μM
Incubation Time:24 h
Result:Significantly increased cGMP levels by about 200% in a dose-dependent manner. Reversed the Aβ-induced decrease in phosphorylated CREB in a dose-dependent manner. Aβ42alone increased the levels of cleaved caspase-3 and cleaved PARP, whereas the combined treatment with mirodenafil markedly reduced the expression levels of both apoptotic markers.

RT-PCR[3]

Cell Line:NIH3T3 mouse embryonic fibroblasts
Concentration:0, 10, 100 μM
Incubation Time:24 h
Result:The mRNA expression of COL1A1, α-SMA, and CTGF were induced by treatment with TGF-β1, and Mirodenafil significantly reduced the expression of these profibrotic genes.
体内研究
(In Vivo)

Mirodenafil (4 mg/kg, IP, daily for 4 weeks) enhances the cognitive-behavioral performance in transgenic AD mice[2].
Mirodenafil (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[3].

Animal Model:APP-C105 transgenic mice (13-month-old, male, n=6)[2]
Dosage:4 mg/kg
Administration:IP, daily for 4 weeks
Result:Improved cognitive function in the APP-C105 AD mice.
Animal Model:Male BALB/c mice (8 weeks old, four groups, n=10/group)[3]
Dosage:0, 5 or 10 mg/kg
Administration:Orally, daily for 3 weeks
Result:Ameliorated dermal fibrosis and downregulated the protein levels of fibrosis markers including COL1A1 and α-SMA in the BLM-induced SSc mouse model. Significantly decreased dermal thickness and collagen content.
Clinical Trial
分子量

531.67

Formula

C26H37N5O5S

CAS 号

862189-95-5

中文名称

米罗那非

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.