Pimobendan hydrochloride
(Synonyms:匹莫苯丹盐酸盐)
目录号 : KG10642
CAS No. : 77469-98-8
纯度 : 98%
Pimobendan (hydrochloride) (UD-CG115 (hydrochloride)) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Pimobendan (UD-CG115) 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 (IC50 >30 μM). In human atrial cells, 100 μM Pimobendan (UD-CG115) 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 (UD-CG115) increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells.
Pimobendan (UD-CG115) shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan (UD-CG115) significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (UD-CG115) (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 (UD-CG115) suppresses expression of the intracardiac iNOS gene , causing reduction of intracardiac NO production.
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| 分子式 |
C19H19ClN4O2
|
| 分子量 |
370.83
|
| CAS号 |
77469-98-8
|
| 中文名称 |
Pimobendan (hydrochloride)
|
| 储存方式 |
| Powder |
-20°C |
3 years |
| |
4°C |
2 years |
| In solvent |
-80°C |
6 months |
| |
-20°C |
1 month |
|