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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Cinaciguat
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
329773-35-5
- 规格：
50mg/25mg/10mg/5mg/1mg
| 规格： | 50mg | 产品价格： | ￥3340.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2215.0 |
| 规格： | 10mg | 产品价格： | ￥1228.0 |
| 规格： | 5mg | 产品价格： | ￥793.0 |
| 规格： | 1mg | 产品价格： | ￥256.0 |
| 基本信息 | |
| CAS | No.329773-35-5 |
| 英文名称 | Cinaciguat |
| 别名 | BAY 58-2667 |
| 分子式 | C36H39NO5 |
| 分子量 | 565.7 |
| 溶解性 | Soluble in DMSO ≥5mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD18782678 |
| SMILES | C1=CC=C(C=C1)CCC2=CC=C(C=C2)COC3=CC=CC=C3CCN(CCCCC(=O)O)CC4=CC=C(C=C4)C(=O)O |
| InChIKey | WPYWMXNXEZFMAK-UHFFFAOYSA-N |
| InChI | InChI=1S/C36H39NO5/c38-35(39)12-6-7-24-37(26-30-19-21-33(22-20-30)36(40)41)25-23-32-10-4-5-11-34(32)42-27-31-17-15-29(16-18-31)14-13-28-8-2-1-3-9-28/h1-5，8-11，15-22H，6-7，12-14，23-27H2，(H，38，39)(H，40，41) |
| PubChem CID | 9808022 |
| 靶点 | Guanylate Cyclase |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | 是一种不依赖于一氧化氮的鸟苷酸环化酶 (GC) 活化剂。 |
| 生物活性 | Cinaciguat is an activator of guanylate cyclase (sGC)， and used for acute decompensated heart failure.[1][2][3] |
| In Vitro | Here， we analyzed the dose-dependent effects of clinical relevant concentrations (10(-10)-10(-5) M) of the sGC activator cinaciguat and the sGC stimulator riociguat on the contraction， relaxation， and calcium transients of isolated field-stimulated cardiac myocytes from healthy rats. For comparison， we used isoproterenol， which induced a dose-dependent significant increase in cell contractility， relaxation， and calcium transients， verapamil that significantly decreased these parameters (both at 10(-9)-10(-5) M) and 8-(4-Chlorophenylthio)-guanosine 3，5-cyclic monophosphate (8-pCPT-cGMP) that induced a negative inotropic effect at 10(-5) M accompanied by a slight increase in relaxation. In contrast， neither cinaciguat nor riociguat significantly influenced any measured parameters.Furthermore， isoproterenol significantly increased intracellular cAMP levels that were not influenced by cinaciguat or riociguat (all at 10(-6) M). Otherwise， riociguat and cinaciguat (both at 10(-6) M) significantly enhanced intracellular cGMP generation. This accumulation was significantly augmented by cinaciguat in the presence of the sGC inhibitor 1H-[1，2，4]oxadiazolo[4，3-a]quinoxalin-1-one (ODQ， 25 μM)， whereas ODQ blocked cGMP generation by riociguat. However， blocking of sGC did not influence cell contractility.[2]。 |
| 细胞实验 | Type - 1 DM was induced in rats by streptozotocin. Animals were treated either with the sGC activator cinaciguat (10 mg/kg/day) or with placebo orally for 8 weeks.Left ventricular (LV) pressure - volume (P - V) analysis was used to assess cardiac performance. Additionally， gene expression (qRT - PCR) and protein expression analysis (western blot) were performed. Cardiac structure， markers of fibrotic remodelling and DNA damage were examined by histology， immunohistochemistry and TUNEL assay， respectively.DM was associated with deteriorated cGMP signalling in the myocardium (elevated phosphodiesterase - 5 expression， lower cGMP - level and impaired PKG activity). Cardiomyocyte hypertrophy， fibrotic remodelling and DNA fragmentation were present in DM that was associated with impaired LV contractility (preload recruitable stroke work (PRSW): 49.5 ± 3.3 vs. 83.0 ± 5.5 mmHg， P < 0.05) and diastolic function (time constant of LV pressure decay (Tau): 17.3 ± 0.8 vs. 10.3 ± 0.3 ms， P < 0.05). Cinaciguat treatment effectively prevented DM related molecular， histological alterations and significantly improved systolic (PRSW: 66.8 ± 3.6 mmHg) and diastolic (Tau: 14.9 ± 0.6 ms) function.[1]。 |
| 动物实验 | After confirmation of DM， rats are randomised into four groups: vehicle-treated control， cinaciguat-treated control， vehicle-treated diabetic and cinaciguat-treated diabetic groups. Animals are treated for 8 weeks with 0.5% methylcellulose vehicle or with the sGC activator cinaciguat in suspension p.o. (10 mg/kg/day)， starting immeadiately after DM confirmation. Water bottles are filled every morning with the same amount of fresh tap water and daily water intake is measured. Animal cages are handled with care and are not moved after water bottle replacement to prevent spilling of water from the bottles. Body weight of the animals are recorded every 2 days and the dose of cinaciguat is adjusted accordingly. |
| 数据来源文献 | [1]. Mátyás C， et al. The soluble guanylate cyclase activator cinaciguat prevents cardiac dysfunction in a rat model of type-1 diabetes mellitus. Cardiovasc Diabetol. 2015 Oct 31;14:145. [2]. Reinke Y， et al. The soluble guanylate cyclase stimulator riociguat and the soluble guanylate cyclase activator cinaciguat exert no direct effects on contractility and relaxation of cardiac myocytes from normal rats. Format: AbstractSend to Eur J Pharmaco [3]. Cosyns SM， et al. Influence of cinaciguat on gastrointestinal motility in apo-sGC mice. Neurogastroenterol Motil. 2014 Nov;26(11):1573-85. |
| 单位 | 瓶 |
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IC7300 Cinaciguat 代谢酶/蛋白酶 索莱宝
￥256 - 3340
