1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation Stem Cell/Wnt Apoptosis
  2. Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis
  3. Mirodenafil

Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).

For research use only. We do not sell to patients.

Mirodenafil Chemical Structure

Mirodenafil Chemical Structure

CAS No. : 862189-95-5

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Description

Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling 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

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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. Aβ42 alone 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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

531.67

Formula

C26H37N5O5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(N(CC)C=C2CCC)=C2N=C(C3=CC(S(=O)(N4CCN(CCO)CC4)=O)=CC=C3OCCC)N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (235.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8809 mL 9.4043 mL 18.8087 mL
5 mM 0.3762 mL 1.8809 mL 3.7617 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8809 mL 9.4043 mL 18.8087 mL 47.0217 mL
5 mM 0.3762 mL 1.8809 mL 3.7617 mL 9.4043 mL
10 mM 0.1881 mL 0.9404 mL 1.8809 mL 4.7022 mL
15 mM 0.1254 mL 0.6270 mL 1.2539 mL 3.1348 mL
20 mM 0.0940 mL 0.4702 mL 0.9404 mL 2.3511 mL
25 mM 0.0752 mL 0.3762 mL 0.7523 mL 1.8809 mL
30 mM 0.0627 mL 0.3135 mL 0.6270 mL 1.5674 mL
40 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1755 mL
50 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9404 mL
60 mM 0.0313 mL 0.1567 mL 0.3135 mL 0.7837 mL
80 mM 0.0235 mL 0.1176 mL 0.2351 mL 0.5878 mL
100 mM 0.0188 mL 0.0940 mL 0.1881 mL 0.4702 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mirodenafil
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HY-14930
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