NSP-805
目录号 : GC32572NSP-805是一种有效的,选择性的phosphodiesterase3(PDE3)抑制剂,为一种强心剂,具有舒张血管的作用。
Cas No.:125068-54-4
Sample solution is provided at 25 µL, 10mM.
NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
In isolated guinea pig left atria, NSP-805 shows positive inotropic EC50 value in order of potency of 0.18 μM. The in vitro positive inotropic effects of NSP-805 is accompanied by increases in tissue cyclic AMP and abolished by carbachol[1].
In anesthetized dogs, intravenous (i.v.) injection of NSP-805 produces dose-dependent increases in left ventricular VVdp/dtmax and decreases in aortic blood pressure (ABP) with relatively small increases in heart rate (HR). The ED50 value for LVdP/dtmax of NSP-805 is 12 μg/kg. When the drugs is administered intraduodenally to anesthetized dogs, the ED50 value for LVdP/dtmax of NSP-805, is approximately 10 μg/kg. In the propranolol-induced heart failure model, NSP-805 completely improves the hemodynamic state of heart failure to normal levels[1]. NSP-805(100 μg/kg) reduces systemic blood pressure significantly, but the increase of chorio-retinal blood flow is less than that at the low dose of NSP-805 (40 μg/kg) in rabbit eyes[2].
[1]. Mochizuki N, et al. Cardiovascular effects of NSP-804 and NSP-805, novel cardiotonic agents with vasodilator properties. J Cardiovasc Pharmacol. 1993 Jun;21(6):983-95. [2]. Uchida H, et al. [The effect of phosphodiesterase type 3 inhibitor on chorio-retinal blood flow in rabbits eyes]. Nippon Ganka Gakkai Zasshi. 2002 Oct;106(10):615-20.
Cas No. | 125068-54-4 | SDF | |
Canonical SMILES | O=C1CC(C)C(C2=CC=C(NC3=C(C)C(CC3)=O)C=C2)=NN1 | ||
分子式 | C17H19N3O2 | 分子量 | 297.35 |
溶解度 | Soluble in DMSO | 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。 |
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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 | 3.363 mL | 16.8152 mL | 33.6304 mL |
5 mM | 0.6726 mL | 3.363 mL | 6.7261 mL |
10 mM | 0.3363 mL | 1.6815 mL | 3.363 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。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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