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NSP-805 {[allProObj[0].p_purity_real_show]}

货号:A1177318

NSP-805是一种高效、选择性的磷酸二酯酶 3 (PDE3) 抑制剂,具有强心和血管扩张作用,适用于心血管疾病的研究,特别是在治疗心力衰竭和血液循环不良方面有广泛应用。

NSP-805 化学结构 CAS号:125068-54-4
NSP-805 化学结构
CAS号:125068-54-4
NSP-805 3D分子结构
CAS号:125068-54-4
NSP-805 化学结构 CAS号:125068-54-4
NSP-805 3D分子结构 CAS号:125068-54-4
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NSP-805 纯度/质量文件 产品仅供科研

货号:A1177318 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine AChR,mAChR 98%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 98%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

98%
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A1, IC50: 0.7 nM

PDE4A4, IC50: 4.3 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

98+%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

NSP-805 生物活性

描述 In isolated guinea pig left atria, NSP-805 exhibits a positive inotropic EC50 value with a potency order of 0.18 μM. The in vitro positive inotropic effects of NSP-805 are accompanied by increases in tissue cyclic AMP and are abolished by carbachol[1].
体内研究

In anesthetized dogs, intravenous (i.v.) administration of NSP-805 leads to dose-dependent increases in left ventricular VVdp/dtmax and decreases in aortic blood pressure (ABP) with relatively slight increases in heart rate (HR). The ED50 value for LVdP/dtmax of NSP-805 is 12 μg/kg. When 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 restores the hemodynamic state of heart failure to normal levels[1].

NSP-805 (100 μg/kg) significantly reduces systemic blood pressure, but the increase in chorio-retinal blood flow is lower than that observed with the low dose of NSP-805 (40 μg/kg) in rabbit eyes[2].

体外研究

In isolated guinea pig left atria, NSP-805 exhibits a positive inotropic EC50 value with a potency order of 0.18 μM. The in vitro positive inotropic effects of NSP-805 are accompanied by increases in tissue cyclic AMP and are abolished by carbachol[1].

NSP-805 参考文献

[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.

NSP-805 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.82mL

3.36mL

1.68mL

33.63mL

6.73mL

3.36mL

NSP-805 技术信息

CAS号125068-54-4
分子式C17H19N3O2
分子量 297.352
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 40 mg/mL(134.52 mM),配合低频超声助溶,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

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