货号:A157577
同义名:
UD-CG115;UD-CG 115 BS
Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
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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 | ✔ | 99%+ | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
99%+ | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | mAChR,AChR | 99%+ | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 99%+ | |||||||||||||||||
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 | 99%+ | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
99%+ | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
99%+ | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99%+ | ||||||||||||||||
(S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
98% | |||||||||||||||||
Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
Roflumilast |
++++
PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM |
99% | |||||||||||||||||
Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
Cilomilast |
+++
LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM |
98+% | |||||||||||||||||
Avanafil |
++++
PDE5, IC50: 1 nM |
99%+ | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
99%+ | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
99%+ | ||||||||||||||||
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。 |
靶点 |
|
描述 | Ca2+ influx via the L-type calcium current (ICa(L)) is the major factor in the regulation of cardiac excitation-contraction coupling. While ICa(L) is known to be regulated by cAMP-dependent phosphorylation in cardiac tissues. And phosphodiesterase III (PDE III) is specific for the s hydrolysis of cAMP. Pimobendan is a selective inhibitor of PDE III with an IC50 value of 0.32 μM. On average, 1, 10 and 100 μM pimobendan increased ICa(L) by 129.3±20.3% (n=11), 221.5±29.5% (n=12) and 250.4±45.0% (n=15), respectively, in human atrial cells. The maximal effect (Emax) of pimobendan on ICa(L) and for the concentration for half-maximal stimulation (EC50) were 249.4% and 1.13 μM, respectively, in human myocytes [3]. In DBA/2 mice inoculated with the encephalomyocarditis virus, the survival of mice improved in a dose-dependent fashion following orally once daily treatment with pimobendan. And a significant difference (p < 0.02) was found between the higher-dose pimobendan group (20 of 30 [66.7%]) and the control group (11 of 30 [36.7%]). Furthermore, intracardiac NO production was significantly (p < 0.001) less in the pimobendan group (0.165±0.004 nmol/mg heart) than in the control group (0.291±0.051 nmol/mg heart) [4]. |
[1]Beier N, et al. J Cardiovasc Pharmacol, 1991, 18(1), 17-27.
[2]Brunkhorst D, et al. Naunyn Schmiedebergs Arch Pharmacol, 1989, 339(5), 575-583.
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.99mL 0.60mL 0.30mL |
14.95mL 2.99mL 1.50mL |
29.91mL 5.98mL 2.99mL |
CAS号 | 74150-27-9 |
分子式 | C19H18N4O2 |
分子量 | 334.372 |
别名 | UD-CG115;UD-CG 115 BS |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(149.53 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 |
动物实验配方 |
0.5% methylcellulose+water 30 mg/mL suspension |