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Mirodenafil dihydrochloride

Cat. No. M30720
Mirodenafil dihydrochloride Structure
Synonym:

SK-3530 dihydrochloride

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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 604.59
Formula C26H39Cl2N5O5S
CAS Number 862189-96-6
Form Solid
Solubility (25°C) DMSO ≥ 100 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Z R Shodmonova, et al. Urologiia. [Phosphodesterase type 5 inhibitors clinical efficiency and role in therapy for erectile dysfunction]

[2] Riccardo Lombardo, et al. Curr Drug Targets. Phosphodiesterases 5 Inhibitors and Erectile Dysfunction Recovery after Pelvic Surgery: Future Perspectives for New Drugs and New Formulations

[3] Kwangsung Park, et al. Asian J Androl. Prevalence and medical management of erectile dysfunction in Asia

[4] Young S Lee, et al. Biopharm Drug Dispos. Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, in spontaneously or DOCA-salt-induced hypertensive rats

[5] Y S Lee, et al. Xenobiotica. Pharmacokinetics of mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of mirodenafil to streptozotocin-induced diabetes mellitus rats

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