Mirodenafil Dihydrochloride
Mirodenafil Dihydrochloride Basic information
- Product Name:
- Mirodenafil Dihydrochloride
- Synonyms:
-
- Mirodenafil Dihydrochloride
- Mirodenafil dihydrochloride, >=98%
- mirodenafil HCl
- CS-1262
- Mirodenafil-dihydrochloride, SK-3530 dihydrochloride
- 5-Ethyl-3,5-dihydro-2-[5-[[4-(2-hydroxyethyl)-1-piperazinyl]sulfonyl]-2-propoxyphenyl]-7-propyl-4H-pyrrolo[3,2-d]pyriMidin-4-one Hydrochloride
- Mirodenafil hydrocloride
- SK 3530
- CAS:
- 862189-96-6
- MF:
- C26H37N5O5S
- MW:
- 531.66748
- EINECS:
- 1308068-626-2
- Product Categories:
-
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Sulfur & Selenium Compounds
- Mol File:
- 862189-96-6.mol
Mirodenafil Dihydrochloride Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml; Ethanol: 10 mg/ml
- form
- A crystalline solid
- color
- White to off-white
- SMILES
- c1c(OCCC)c(C2NC(=O)c3[n](CC)c-c(CCC)c-3N=2)cc(S(=O)(=O)N2CCN(CCO)CC2)c1
Mirodenafil Dihydrochloride Usage And Synthesis
Uses
Mirodenafil, a phosphodiesterase 5 inhibitor reported to be effective in the treatment of erectile dysfunction, is metabolized by cytochrome P 450 (CYP) 3A4 to the active metabolite N-dehydroxyethyl mirodenafil. Mirodenafil may have drug-drug interactions with ketoconazole and/or rifampicin.
Biological Activity
Mirodenafil (SK3530) is an orally active, highly potent and selective phosphodiesterase-5 (PDE5) inhibitor (IC50 = 338 pM). with therapeutic efficacy in various ED models in vivo. Comparing to sildenafil, mirodenafil shows ~10-times higher PDE5 selectivity in vitro and remains longer in the plasma and corpus cavernosum following oral dosing at 40 mg/kg in rats in vivo.
in vivo
Mirodenafil dihydrochloride (4 mg/kg, IP, daily for 4 weeks) enhances the cognitive-behavioral performance in transgenic AD mice[2].
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[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. |
IC 50
PDE5
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