Mirodenafil dihydrochloride
(Synonyms: 米罗那非二盐酸盐,SK-3530 dihydrochloride) 目录号 : GC36617
A PDE5 inhibitor
Cas No.:862189-96-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mirodenafil is a phosphodiesterase 5 (PDE5) inhibitor.1 It increases penile intracavernosal pressure (ICP) in a rat model of diabetes induced by streptozotocin and in a rat model of cavernosal nerve injury when administered at doses of 1 and 10 mg/kg, respectively.1,2 Mirodenafil (4 mg/kg per day) decreases bladder wall submucosal fibrosis and degeneration in a rat model of chronic bladder ischemia.3 It also decreases bladder overactivity in a female rat model of partial bladder outlet obstruction.4
1.Park, K., Cho, S.Y., and Kim, S.W.Erectile response to type 5 phosphodiesterase inhibitor could be preserved with the addition of simvastatin to conventional insulin treatment in rat model of diabetesInt. J. Androl.34(5 Pt 2)e468-e474(2011) 2.Kim, H., Sohn, D.W., Kim, S.D., et al.The effect of mirodenafil on the penile erection and corpus cavernosum in the rat model of cavernosal nerve injuryInt. J. Impot. Res.22(5)291-297(2010) 3.Choi, H., Bae, J.H., Shim, J.S., et al.Mirodenafil prevents bladder dysfunction induced by chronic bladder ischemia in ratsInt. Neurourol. J.19(1)19-26(2015) 4.Kang, J.Y., Kim, E.K., and Kim, K.M.Effects of mirodenafil, a phosphodiesterase-5 inhibitor, on female rat bladder in a partial bladder outlet obstruction model: Physiological and immunohistochemical aspectsKorean J. Urol.54(5)339-344(2013)
| Cas No. | 862189-96-6 | SDF | |
| 别名 | 米罗那非二盐酸盐,SK-3530 dihydrochloride | ||
| Canonical SMILES | [H]Cl.[H]Cl.O=C1C(N(CC)C=C2CCC)=C2N=C(C3=CC(S(=O)(N4CCN(CCO)CC4)=O)=CC=C3OCCC)N1 | ||
| 分子式 | C26H39Cl2N5O5S | 分子量 | 604.59 |
| 溶解度 | DMSO: ≥ 100 mg/mL (165.40 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.654 mL | 8.2701 mL | 16.5401 mL |
| 5 mM | 0.3308 mL | 1.654 mL | 3.308 mL |
| 10 mM | 0.1654 mL | 0.827 mL | 1.654 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pharmacokinetics of Mirodenafil and its two metabolites, SK3541 and SK3544, in spontaneously or DOCA-salt-induced hypertensive rats
Biopharm Drug Dispos 2011 Jan;32(1):38-49.PMID:21162118DOI:10.1002/bdd.737.
Hypertension is the most common comorbidity and major risk factor in patients with erectile dysfunction. The pharmacokinetics of Mirodenafil, used for the treatment of erectile dysfunction, after the intravenous and oral administration (20 mg/kg) to 6-week-old rats (with blood pressure within the normotensive range) and 16-week-old spontaneously hypertensive rats (SHRs) and their age-matched control normotensive Kyoto-Wistar (KW) rats, and 16-week-old deoxycorticosterone acetate-salt-induced hypertensive rats (DOCA-salt rats) and their age-matched control Sprague-Dawley (SD) rats were compared. It was found that time-averaged renal clearance (Cl(r)) was of minor importance and that time-averaged non-renal clearance (Cl(nr)) was dominant. In both 6- and 16-week-old SHRs, the Cl(nr)s and areas under the curve (AUCs) of intravenous Mirodenafil were significantly smaller and greater than those of the controls, but in 16-week-old DOCA-salt rats, they were comparable to the controls. Although the AUC of oral Mirodenafil in 16-week-old SHRs was comparable to the controls, the Cl(nr)s (or total body clearances, Cls) of intravenous Mirodenafil and intestinal intrinsic clearances were significantly smaller than the controls and comparable to the controls for both 6- and 16-week-old SHRs, unlike in the 16-week-old DOCA-salt rats. The above data suggest that the significantly smaller Cl(nr) and greater AUC of intravenous Mirodenafil and comparable AUC of oral Mirodenafil in 16-week-old SHR could be due to the hereditary characteristics of SHRs, and not due to the hypertensive state itself.
Pharmacokinetics of Mirodenafil and its two metabolites, SK3541 and SK3544, after intravenous and oral administration of Mirodenafil to streptozotocin-induced diabetes mellitus rats
Xenobiotica 2010 Feb;40(2):129-37.PMID:19929308DOI:10.3109/00498250903380975.
The area under the curve (AUC) of Mirodenafil after intravenous administration in diabetes mellitus induced by streptozotocin (DMIS) rats was significantly smaller (by 28.0 %) than the control value, and the AUC(SK3541)/AUC(Mirodenafil) ratio was significantly greater (by 130 %) in DMIS rats. This may be explained by the significantly faster hepatic CL(int) of Mirodenafil, owing to increased hepatic CYP1A, CYP2B1/2, CYP2D, and CYP3A expression, and a faster hepatic blood flow rate, compared with control values. The AUC of Mirodenafil after oral administration was comparable between DMIS and control rats, possibly because of the comparable intestinal CL(int), which may be attributable to increased CYP1A2 expression and decreased CYP2D expression in the intestines of DMIS rats.
Prevalence and medical management of erectile dysfunction in Asia
Asian J Androl 2011 Jul;13(4):543-9.PMID:21460862DOI:10.1038/aja.2010.131.
Erectile dysfunction (ED) is an important worldwide health issue that has a significant negative impact on the quality of life and life satisfaction of both the affected individual and his partner. Here we review the prevalence of ED in Asia, associated factors that may influence sexual attitudes and sexual behaviours, and randomized clinical trials (RCTs) of phosphodiesterase-5 (PDE-5) inhibitors to evaluate the clinical efficacy and safety of PDE-5 inhibitors in Asian men. We searched for English-language articles in MEDLINE and PubMed from January 2000 to September 2010. Our results showed that the overall reported prevalence rate of ED in Asia ranged widely, from 2% to 88%. This finding indicates that ED is a common and major health problem in this region. However, sociocultural and economic factors in Asia prevent people from seeking and obtaining appropriate medical care. We found reports on five kinds of PDE-5 inhibitors for the management of ED: sildenafil, vardenafil, tadalafil, udenafil and Mirodenafil. The results of RCTs showed that these five PDE-5 inhibitors are more effective than placebo in improving erectile function in Asian men with ED and that these drugs have similar efficacy and safety profiles.
Phosphodiesterases 5 Inhibitors and Erectile Dysfunction Recovery after Pelvic Surgery: Future Perspectives for New Drugs and New Formulations
Curr Drug Targets 2021;22(1):31-37.PMID:32981502DOI:10.2174/1389450121666200925145347.
Background: Phosphodiesterase 5 inhibitors (PDE5I) represent the first-line treatment in the management of post-operative erectile dysfunction (ED) after pelvic oncological surgery. The aim of our study is to evaluate the available evidence on the efficacy of PDE5Is, including new formulations and penile rehabilitation post-pelvic surgery. Evidence acquisition: A systematic review of the literature was performed until May 2020. The following databases were searched: Scopus, Medline and Web of Science. The MeSH search was conducted by combining the following terms: 'erectile dysfunction', 'radical prostatectomy' 'pelvic' 'bladder' 'phosphodiesterase' inhibitors' 'avanafil' 'sildenafil' 'tadalafil' 'lodenafil' 'Mirodenafil' 'udenafil' 'vardenafil' 'sublingual' 'orodispersible' 'penile' 'rehabilitation'. Evidence synthesis: Sildenafil, Tadalafil, vardenafil and Avanafil improve EF compared with placebo in men with all levels of ED severity after radical prostatectomy with good tolerability. No specific recommendations can be suggested regarding the superiority of a drug over the other. The optimal dose, continuous vs. on-demand and duration of treatment, is still under investigation. In vitro and preclinical studies suggest the possible role for lodenafil, Mirodenafil and oro-dispersible formulations in patients undergoing oncological pelvic surgery. Few studies demonstrated the efficacy of udenafil in improving ED after rectal surgery or radical prostatectomy. Complete recovery of EF after surgery is still an unmet need in the field of penile rehabilitation after pelvic surgery. Conclusion: PDE5Is have a crucial role in the management of post pelvic surgery of ED. New drugs and new formulations have shown excellent results in patients with ED; however, data in patients after surgery is still scarce. Further well designed RCT should clarify the role of these new compounds and oro-dispersible formulations in the management of ED in patients undergoing pelvic surgery.
[Phosphodesterase type 5 inhibitors clinical efficiency and role in therapy for erectile dysfunction]
Urologiia 2021 May;(2):135-140.PMID:33960173doi
This article discusses the physiological mechanisms of erection and the pathophysiological basis of erectile dysfunction. Parameters characterizing the features of the pharmacokinetics and pharmacodynamics of drugs from the group of phosphodiesterase type 5 inhibitors (PDE-5i) are presented. The clinical efficacy and possible adverse effects of the most significant PDE-5i are considered. These include sildenafil, tadalafil, vardenafil, udenafil, avanafil. There are also data on less known PDE-5i, which include lodenafil and Mirodenafil.