| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
The neuroprotective effects of mirodenafil diHClide (0-40 μM, 24 h) are achieved through the activation of the cGMP/PKG/CREB signaling pathway [2]. Through the inhibition of apoptosis and preservation of mitochondrial membrane potential, mirodenafil diHClide (0–40 μM, 24 hours) improves neuronal survival [2]. Mirodenafil diHClide (0–40 μM) suppresses GSK-3β signaling, which lowers tau phosphorylation and reduces the generation of Aβ by blocking the formation of amyloid and triggering the autophagosome pathway [2]. In HT-22 cells, mirodenafil diHClide prevents GR homodimerization and the transcriptional activity of the glucocorticoid receptor (GR) [2]. In fibroblasts, mirodenafil diHClide (0-100 μM, 24 h) suppresses the production of the fibrosis marker mRNA and Smad2/3 phosphorylation produced by TGF-β [3].
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| ln Vivo |
The behavioral and cognitive abilities of transgenic AD mice can be improved by administering 4 mg/kg of mildenafil hydrochloride intraperitoneally once a day for 4 weeks [2]. By reducing the expression of profibrotic genes and collagen, mirodenafil diHClide (0-10 mg/kg) oral daily for three weeks improves the BLM-induced SSc mice model. This is achieved by blocking the TGF-β signaling pathway. Fibrosis of the skin[3].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: SH-SY5Y Human Neuroblastoma Cells Tested Concentrations: 0, 10, 20, 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: cGMP levels were Dramatically increased by approximately 200% in a dose-dependent manner. Reversal of Aβ-induced reduction in phosphorylated CREB in a dose-dependent manner. Aβ42 alone increased the levels of cleaved caspase-3 and cleaved PARP, whereas combined treatment with mironafil Dramatically diminished the expression levels of both apoptotic markers. RT-PCR[3] Cell Types: NIH3T3 mouse embryonic fibroblasts Tested Concentrations: 0, 10, 100 μM Incubation Duration: 24 h Experimental Results: TGF-β1 induced COL1A1, α-SMA and CTGF mRNA expression, and midenafil Dramatically diminished the expression of these profibrotic genes. |
| Animal Protocol |
Animal/Disease Models: APP-C105 transgenic mice (13 months old, male, n=6) [2]
Doses: 4 mg/kg Route of Administration: intraperitoneal (ip) injection, one time/day for 4 weeks Experimental Results: APP-C105 AD The mice's cognitive function improved. Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (8 weeks old, four groups, n=10/group) [3] Doses: 0, 5 or 10 mg/kg Route of Administration: Orally, one time/day for 3 weeks Experimental Results: Improved dermal fibrosis and downregulated protein levels of fibrosis markers, including COL1A1 and α-SMA, in BLM-induced SSc mouse model. Dermal thickness and collagen content were Dramatically diminished. |
| References |
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| Molecular Formula |
C26H39CL2N5O5S
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|---|---|
| Molecular Weight |
604.588
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| Exact Mass |
603.205
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| CAS # |
862189-96-6
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| Related CAS # |
Mirodenafil;862189-95-5
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| PubChem CID |
135564928
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| Appearance |
White to off-white solid powder
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| LogP |
5.424
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
39
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| Complexity |
902
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CKPHITUXXABKDL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H37N5O5S.2ClH/c1-4-7-19-18-30(6-3)24-23(19)27-25(28-26(24)33)21-17-20(8-9-22(21)36-16-5-2)37(34,35)31-12-10-29(11-13-31)14-15-32/h8-9,17-18,32H,4-7,10-16H2,1-3H3,(H,27,28,33)2*1H
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| Chemical Name |
5-Ethyl-2-[5-[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl-2-propoxyphenyl]-7-propyl-1H-pyrrolo[3,2-d]pyrimidin-4-one dihydrochloride
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| Synonyms |
Mirodenafil Dihydrochloride SK3530 M-vix SK-3530SK-3530 dihydrochloride SK 3530
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~165.40 mM)
H2O : ~5 mg/mL (~8.27 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6540 mL | 8.2701 mL | 16.5401 mL | |
| 5 mM | 0.3308 mL | 1.6540 mL | 3.3080 mL | |
| 10 mM | 0.1654 mL | 0.8270 mL | 1.6540 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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