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Pimobendan

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Chemical Structure| 74150-27-9 同义名 : UD-CG115;UD-CG 115 BS
CAS号 : 74150-27-9
货号 : A157577
分子式 : C19H18N4O2
纯度 : 98%
分子量 : 334.372
MDL号 : MFCD00761648
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

生物活性
靶点

  • PDE3

    PDE3, IC50:0.32 μM
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].
实验方案
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
参考文献

[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.

[3]Kajimoto K, Hagiwara N, Kasanuki H, Hosoda S. Contribution of phosphodiesterase isozymes to the regulation of the L-type calcium current in human cardiac myocytes. Br J Pharmacol. 1997 Aug;121(8):1549-56. doi: 10.1038/sj.bjp.0701297. PMID: 9283687; PMCID: PMC1564856.

[4]Iwasaki A, Matsumori A, Yamada T, Shioi T, Wang W, Ono K, Nishio R, Okada M, Sasayama S. Pimobendan inhibits the production of proinflammatory cytokines and gene expression of inducible nitric oxide synthase in a murine model of viral myocarditis. J Am Coll Cardiol. 1999 Apr;33(5):1400-7. doi: 10.1016/s0735-1097(98)00692-5. PMID: 10193745.