| Identification | Back Directory | [Name]
Mirodenafil Dihydrochloride | [CAS]
862189-96-6 | [Synonyms]
CS-1262
SK 3530
mirodenafil HCl
SK-3530 dihydrochloride
Mirodenafil hydrocloride
Mirodenafil Dihydrochloride
Mirodenafil (hydrochloride)
Mirodenafil dihydrochloride, >=98%
mirodenafil HCl salt ,Mirodenafil Dihydrochloride
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 | [EINECS(EC#)]
1308068-626-2 | [Molecular Formula]
C26H37N5O5S | [MDL Number]
MFCD28139019 | [MOL File]
862189-96-6.mol | [Molecular Weight]
531.667 |
| Chemical Properties | Back Directory | [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 | [InChIKey]
CKPHITUXXABKDL-UHFFFAOYSA-N | [SMILES]
c1c(OCCC)c(C2NC(=O)c3[n](CC)c-c(CCC)c-3N=2)cc(S(=O)(=O)N2CCN(CCO)CC2)c1 |
| Hazard Information | Back Directory | [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 activehighly potent and selective phosphodiesterase-5 (PDE5) inhibitor (IC50 = 338 pM). with therapeutic efficacy in various ED models in vivo. Comparing to sildenafilmirodenafil 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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