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Mirodenafil

CAS# 862189-95-5

Mirodenafil

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Chemical structure

Mirodenafil

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Chemical Properties of Mirodenafil

Cas No. 862189-95-5 SDF Download SDF
PubChem ID 12001014 Appearance Powder
Formula C26H37N5O5S M.Wt 531.67
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
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
SMILES CCCC1=CN(C2=C1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CCO)OCCC)CC
Standard InChIKey MIJFNYMSCFYZNY-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H37N5O5S/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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Mirodenafil Dilution Calculator

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Mirodenafil Molarity Calculator

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Preparing Stock Solutions of Mirodenafil

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8809 mL 9.4043 mL 18.8087 mL 37.6173 mL 47.0216 mL
5 mM 0.3762 mL 1.8809 mL 3.7617 mL 7.5235 mL 9.4043 mL
10 mM 0.1881 mL 0.9404 mL 1.8809 mL 3.7617 mL 4.7022 mL
50 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.7523 mL 0.9404 mL
100 mM 0.0188 mL 0.094 mL 0.1881 mL 0.3762 mL 0.4702 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Mirodenafil

A review of the efficacy and safety of mirodenafil in the management of erectile dysfunction.[Pubmed:27034723]

Ther Adv Urol. 2016 Apr;8(2):100-17.

Erectile dysfunction (ED) is a common disorder that can jeopardize quality of life and the partnership of patients and their sexual partners. The advent of oral phosphodiesterase type 5 inhibitors (PDE5Is) has revolutionized a treatment for ED, and they are recognized as the first-line therapy for ED, regardless of its etiology. Mirodenafil, a second-generation PDE5I, has biochemical profiles such as high affinity for PDE5 and high selectivity for PDE5 over other PDE isoforms, compared to other existing PDE5Is such as sildenafil, vardenafil and tadalafil. Available evidence has suggested that doses of 50 and 100 mg Mirodenafil effectively improve ED [with improvements in the erectile function domain of the International Index of Erectile Function (IIEF-EF) scores, positive responses to questions 2 of the Sexual Encounter Profiles (SEP2) and questions 3 of the Sexual Encounter Profiles (SEP3): 7.6-11.6 points, 27.72-38.98% and 44.20-67.33%, respectively] in a broad range of patient populations with ED of a variety of underlying etiologies, severities and ages, without any serious treatment-related adverse effects. In the treatment of diabetic ED, a traditionally difficult-to-treat population, 100 mg Mirodenafil has been reported to offer favorable efficacy (with improvements in the IIEF-EF scores, and positive responses to the SEP2 and the SEP3: 9.3 points, 36.1% and 61.8%, respectively) and tolerability (mild adverse effects of less than 19.6%), which are comparable with results from clinical studies on other PDE5Is. Mirodenafil appears to be effective, safe and well tolerated in men with both ED and hypertension or lower urinary tract symptoms (LUTS)/benign prostatic hyperplasia (BPH) who are taking concomitant antihypertensive medications or alpha1-blockers. Furthermore, recent evidence has indicated that Mirodenafil may be a potential option for chronic dosing in the treatment of ED despite its short half-life (T 1/2). Most of the available clinical studies have reported that adverse effects (up to 53.7%) caused by 50 and 100 mg Mirodenafil are mild or moderate in severity, with headache (1.8-14.8%) and flushing (6.7-24.1%) being the most common. Due to the pharmacodynamic profiles of Mirodenafil, its tolerability is expected to be somewhat better than those of the other PDE5Is. However, further well designed studies with larger cohorts of different ethnicities, flexible dosing schedules and long-term follow up are necessary to confirm the favorable efficacy and tolerability profiles of Mirodenafil for the treatment of ED.

The efficacy of mirodenafil for chronic prostatitis/chronic pelvic pain syndrome in middle-aged males.[Pubmed:25606563]

World J Mens Health. 2014 Dec;32(3):145-50.

PURPOSE: The aim of this study was to investigate the efficacy of Mirodenafil in middle-aged male patients with chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS). MATERIALS AND METHODS: Eighty-eight males with CP/CPPS were randomized to receive either levofloxacin (500 mg/d) (group L, 40 patients) or levofloxacin (500 mg/d) and Mirodenafil (50 mg/d) (group ML, 48 patients) for six weeks. The International Prostate Symptom Score (IPSS), National Institutes of Health Chronic Prostatitis Symptom Index (NIH-CPSI), and erectile function (EF) domain scores of the International Index of Erectile Function (IIEF) questionnaire were used to grade symptoms at baseline and 6 weeks after treatment. RESULTS: The mean change in total IPSS from baseline was higher in group ML than that in group L (group L, -1.1 vs. group ML, -4.3; p<0.05). Significant improvements were also seen in the IPSS voiding subscore (group L, -0.7 vs. group ML, -3.0; p<0.05). Changes observed in the NIH-CPSI of group ML at six weeks were greater than those at baseline (group L, -3.2 vs. group ML, -7.2; p<0.05). Significant improvements were seen in the NIH-CPSI voiding (group L, -0.5 vs. group ML, -1.7; p<0.05) and quality of life domains (group L, -1.0 vs. group ML, -1.8; p<0.05). Group ML showed a significantly greater increase in the IIEF-EF score than did group ML (group L, +0.2 vs. group ML, +7.8; p<0.05). CONCLUSIONS: Mirodenafil (50 mg once daily) was well tolerated and resulted in significant symptomatic improvement in middle-aged males with CP/CPPS.

Mirodenafil prevents bladder dysfunction induced by chronic bladder ischemia in rats.[Pubmed:25833477]

Int Neurourol J. 2015 Mar;19(1):19-26.

PURPOSE: To investigate the protective effect of Mirodenafil on bladder function in a rat model of chronic bladder ischemia (CBI). METHODS: Twenty-four Sprague-Dawley rats were randomized to three groups: untreated, sham-operated rats (control group); untreated, CBI model rats (CBI group); and CBI rats treated daily with 4 mg/kg Mirodenafil (CBI+Mirodenafil group). The CBI and CBI+Mirodenafil groups underwent endothelial injury to the iliac arteries and were fed a 2% cholesterol diet after injury. Four weeks after surgery, the CBI+Mirodenafil group started daily treatment with Mirodenafil for four weeks. Eight weeks after surgery, continuous in vivo cystometry and in vivo organ bath studies of detrusor muscle strips were performed. RESULTS: in vivo cystometry revealed that the rats in the CBI group had a significantly higher micturition frequency, lower bladder capacity, and lower compliance than the rats in the control and CBI+Mirodenafil groups. The detrusor muscle strip study showed that the magnitude of the carbachol-induced contractile response was significantly lower in the CBI group compared to either the control or CBI+Mirodenafil group. Addition of daily Mirodenafil after induction of CBI decreased the contractile response, compared to untreated CBI rats. CBI induced submucosal fibrosis and degenerative changes in bladder walls, which was reversed by the addition of Mirodenafil. CONCLUSIONS: Daily treatment with Mirodenafil showed protective effects against bladder dysfunction resulting from CBI in rats.

Drug Concentration in Rat Plasma, Bladder, and Prostate After Mirodenafil Administration in a Chronic Pelvic Ischemia Model.[Pubmed:26919966]

Urology. 2016 May;91:244.e1-5.

OBJECTIVE: To evaluate the distribution of a daily phosphodiesterase type 5 inhibitor dose (Mirodenafil) in rat plasma and bladder and prostate tissue in a model of atherosclerosis-induced chronic pelvic ischemia. METHODS: Thirty-two 18-week-old male Sprague Dawley rats were divided into two groups. Group I (n = 16) comprised a chronic pelvic ischemia model treated with Mirodenafil and group II (n = 16) comprised a sham-operated model also treated with Mirodenafil. The Mirodenafil concentrations in each organ were measured at specific time points after 14 days of daily Mirodenafil administration. The drug distribution ratio of group I to group II of each organ was measured, and the bladder tissue-to-plasma and prostate tissue-to-plasma ratios were calculated. RESULTS: The mean drug concentration in the bladder of the rats in group I did not differ significantly from that of group II after Mirodenafil administration. In the prostate, the mean drug concentration of group I was significantly higher than that of group II at 1 and 4 hours after drug administration. The drug concentration was higher in the bladder tissue than in the prostate tissue and the bladder tissue-to-plasma ratio was significantly higher than the prostate tissue-to-plasma ratio. CONCLUSION: Our results suggest that Mirodenafil levels might be sufficient in the target tissue after daily treatment in an ischemia-induced aging model. Considering the difficulties of tissue distribution study in human subjects, the results of this investigation provided meaningful evidence of the application of daily doses of Mirodenafil for treating lower urinary tract symptoms in an aging population.

Description

Mirodenafil(SK3530) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.

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