Pimobendan (Synonyms: UD-CG 115) |
| رقم الكتالوجGC12808 |
An inhibitor of PDE3
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 74150-27-9
Sample solution is provided at 25 µL, 10mM.
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Pimobendan (UD-CG115) 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[1].
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[2].
References:
[1]. Kajimoto K, et al. 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.
[2]. Iwasaki A, et al. 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.
Animal experiment: | Mice[2]Since, in this model, most mice die of congestive heart failure within 14 days after EMC virus inoculation (21), the survival was observed up to 14 days in this study. Pimobendan was administered in doses of 0.1 mg/kg or 1 mg/kg daily for 14 days from the day of EMC virus inoculation while control mice received vehicles only. Thirty mice were randomly assigned to each group[2]. |
References: [1]. Kajimoto K, et al. 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. | |
| Cas No. | 74150-27-9 | SDF | |
| المرادفات | UD-CG 115 | ||
| Chemical Name | 3-[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one | ||
| Canonical SMILES | CC1CC(=O)NN=C1C2=CC3=C(C=C2)N=C(N3)C4=CC=C(C=C4)OC | ||
| Formula | C19H18N4O2 | M.Wt | 334.37 |
| الذوبان | ≥ 16.2 mg/mL in DMSO, ≥ 19.48 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9907 mL | 14.9535 mL | 29.907 mL |
| 5 mM | 598.1 μL | 2.9907 mL | 5.9814 mL |
| 10 mM | 299.1 μL | 1.4953 mL | 2.9907 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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