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产地 | 中国 |
品牌 | Chemstan |
货号 | LC-01 |
用途 | 中间体 |
包装规格 | 20mg |
纯度 | 98%% |
CAS编号 | 74150-27-9 |
是否进口 | 否 |
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Fields of Application :
Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
CAS Number: | 74150-27-9 |
Purity: | >98% |
Molecular Weight: | 334.37 |
Molecular Formula: | C19H18N4O2 |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
Synonyms: | Vetmedin; Acardi; pimobendane |
Chemical Name: | 6-(2-(4-methoxyphenyl)-1H-benzo[d]imidazol-5-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one |
Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). Pimobendan inhibits the activity of cAMP-PDE III with IC50 of 2.4 μM. It also exerts concentration-dependent positive inotropic effects in isolated guinea-pig papillary muscles with a potency (EC50) of 6.0 μM, which is partly due to selective cardiac PDE III inhibition. In human atrial cells, 100 μM pimobendan significantly increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50) of 1.13 μM. In rabbit atrial cells, Pimobendan increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells Pimobendan shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (1 mg/kg) also significantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with the control group, which shows no effect on myocardial necrosis, heart weight and body weight. Pimobendan suppresses expression of the intracardiac iNOS gene, causing reduction of intracardiac NO production. For the detailed information of Pimobendan, the solubility of Pimobendan in water, the solubility of Pimobendan in DMSO, the solubility of Pimobendan in PBS buffer, the animal experiment (test) of Pimobendan, the cell expriment (test) of Pimobendan, the in vivo, in vitro and clinical trial test of Pimobendan, the EC50, IC50,and Affinity of Pimobendan.
References:
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