产品说明书

Molsidomine

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Chemical Structure| 25717-80-0 同义名 : SIN-10;Morsydomine;N-(Ethoxycarbonyl)-3-(4-morpholinyl)sydnone imine;Corvaton
CAS号 : 25717-80-0
货号 : A335612
分子式 : C9H14N4O4
纯度 : 98%
分子量 : 242.232
MDL号 : MFCD00869301
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(433.47 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(103.21 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Molsidomine is a long-acting vasodilating drug used to treat angina pectoris. Acute treatment with either molsidomine (10 mg/kg body weight, i.v.) or sildenafil (0.7 mg/kg body weight, i.v.) significantly reduced infarct size in normoxic rats and further enhanced cardioprotection induced by CH (chronic hypoxia)[3]. Treatment with molsidomine (5 mg/kg po and 10 mg/kg po) significantly improved motor coordination, paw withdrawal threshold, mechanical threshold, and nerve conduction velocity. Furthermore, molsidomine treatment also reduced malondialdehyde levels and prevented depletion of reduced glutathione in the sciatic nerve homogenate[4]. Molsidomine (5 and 10 mg/kg; p.o.) treatment significantly improved vital sign, renal functions, and oxidative stress in DN rats in a dose-dependent manner[5]. Moreover, intrarenal administration of molsidomine (4 mg/kg) before reperfusion improved renal function and decreased inflammatory responses after I-R(Ischemia reperfusion)[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00382421 Myocardial Ischemia Not Applicable Completed - Switzerland ... 展开 >> Department of Cardiology, Hospital Lucerne Lucerne, Switzerland, 6000 收起 <<
NCT01363661 Stable Angina Pectoris ... 展开 >> Atherosclerosis 收起 << Phase 4 Completed - Belgium ... 展开 >> Onze Lieve Vrouw Ziekenhuis Aalst, Belgium, 9300 收起 <<
NCT01363661 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.64mL

4.13mL

2.06mL

41.28mL

8.26mL

4.13mL

参考文献

[1]Żorniak M, Mitrega KA, et al. New approach to molsidomine active metabolites coming from the results of 2 models of experimental cardiology. Can J Physiol Pharmacol. 2017 Feb;95(2):111-121.

[2]Shan Y, Wang D, et al. Molsidomine Attenuates Ventricular Electrical Remodeling and Arrhythmogenesis in Rats With Chronic β-Adrenergic Receptor Activation Through the NO/cGMP/PKG Pathway. J Cardiovasc Pharmacol. 2016 Nov;68(5):342-355.

[3]Alánová P, Kolář F, Oštádal B, Neckář J. Role of NO/cGMP signaling pathway in cardiac ischemic tolerance of chronically hypoxic rats. Physiol Res. 2015;64(5):783-7

[4]Nayak B P, Minaz N, Pasha K. Molsidomine ameliorates diabetic peripheral neuropathy complications in Wistar rats. Animal Model Exp Med. 2021 Mar 23;4(3):243-248

[5]Minaz N, Razdan R. Therapeutic insight into molsidomine, a nitric oxide donor in streptozotocin-induced diabetic nephropathy in rats. Indian J Pharmacol. 2016 Sep-Oct;48(5):544-549

[6]Rodriguez-Peña A, Garcia-Criado FJ, Eleno N, Arevalo M, Lopez-Novoa JM. Intrarenal administration of molsidomine, a molecule releasing nitric oxide, reduces renal ischemia-reperfusion injury in rats. Am J Transplant. 2004 Oct;4(10):1605-13