Mirodenafil
Based on 1 Customer Validation
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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- No. CAS: 862189-95-5
- Fòrmula: C26H37N5O5S
- Peso molecular:531.67
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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PDE5 |
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.
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Cell Line:SH-SY5Y human neuroblastoma cells
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Concentration:0, 10, 20, 40 μM
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Incubation Time:24 h
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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.
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Cell Line:NIH3T3 mouse embryonic fibroblasts
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Concentration:0, 10, 100 μM
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Incubation Time:24 h
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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.
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.
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Animal Model:APP-C105 transgenic mice (13-month-old, male, n=6)[2]
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Dosage:4 mg/kg
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Administration:IP, daily for 4 weeks
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Result:Improved cognitive function in the APP-C105 AD mice.
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Animal Model:Male BALB/c mice (8 weeks old, four groups, n=10/group)[3]
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Dosage:0, 5 or 10 mg/kg
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Administration:Orally, daily for 3 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 862189-95-5
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Appearance Solid
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Peso molecular 531.67
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Fòrmula C26H37N5O5S
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Color White to off-white
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SMILES
O=C1C(N(CC)C=C2CCC)=C2N=C(C3=CC(S(=O)(N4CCN(CCO)CC4)=O)=CC=C3OCCC)N1
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Synonyms
SK3530
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[3]. Roh JS, et al. Mirodenafil ameliorates skin fibrosis in bleomycin-induced mouse model of systemic sclerosis. Anim Cells Syst (Seoul). 2021 Nov 3;25(6):387-395. [Content Brief]
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 |
Mirodenafil Related Classifications
HY-14930 Related Classifications
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