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Purity: ≥98%
Pimobendan (UD-CG115; UDCG115; Trade names Vetmedin, Acardi), a veterinary medication approved to treat CHF-congestive heart failure in dogs, is a potent and selective inhibitor of phosphodiesterase PDE3 with positive inotropic and vasodilator effects. It inhibits PDE3 with an IC50 of 0.32 μM.
| ln Vitro |
Pimobendan (UD-CG115) selectively inhibits PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to PDE I and PDE II (IC50 >30 μM). In human atrial cells, 100 μM Pimobendan (UD-CG115) considerably increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% at a half-maximal stimulation (EC50) of 1.13 μM. Pimobendan (UD-CG115) elevates ICa(L) at +10 mV by 67.4% in rabbit atrial cells, which is much lower than that observed in human atrial cells[1].
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| ln Vivo |
In the mouse model of EMC virus-induced myocarditis, pimobendan (UD-CG115) has a positive impact on survival. The ultimate survival rate rises dramatically with the administration of pimobendan (UD-CG115), rising from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Comparing the pimobendan (UD-CG115) (1 mg/kg) group to the control group, which has no effect on myocardial necrosis, heart weight, or body weight, reveals a substantial reduction in intracardiac tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and myocardial cellular infiltration. Reduced intracardiac NO generation results from pimobendan (UD-CG115)'s suppression of intracardiac iNOS gene expression[2].
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| Additional Infomation |
Pimobendan is a pyridazinone and a member of benzimidazoles. It has a role as a cardiotonic drug, a vasodilator agent and an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor.
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| Molecular Formula |
C19H18N4O2
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|---|---|
| Molecular Weight |
334.37
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| Exact Mass |
334.142
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| CAS # |
74150-27-9
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| Related CAS # |
Pimobendan hydrochloride;77469-98-8
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| PubChem CID |
4823
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
249 °C(dec.)
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| Index of Refraction |
1.693
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| LogP |
1.81
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
530
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GLBJJMFZWDBELO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N4O2/c1-11-9-17(24)22-23-18(11)13-5-8-15-16(10-13)21-19(20-15)12-3-6-14(25-2)7-4-12/h3-8,10-11H,9H2,1-2H3,(H,20,21)(H,22,24)
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| Chemical Name |
3-[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one
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| Synonyms |
UD-CG-115; UD-CG115; UD CG115; UD-CG 115; Pimobendan; pimobendane. Trade names: Vetmedin and Acardi
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (8.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (8.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (8.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9907 mL | 14.9535 mL | 29.9070 mL | |
| 5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL | |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9907 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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