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Pimobendan

Pimobendan Structure
CAS No.
74150-27-9
Chemical Name:
Pimobendan
Synonyms
VetMedin;(5RS)-6-[2-(4-Methoxyphenyl)-1H-benzimidazol-5-yl]-5- methyl-4,5-dihydropyridazin-3(2H)-one;Acardi;UD-CG 115;PIMOBENDAN;Pimobendam;Pimobendane;UD-CG 115BS;Pimobendanum;PiMobendan EP
CBNumber:
CB6472876
Molecular Formula:
C19H18N4O2
Molecular Weight:
334.37
MOL File:
74150-27-9.mol
MSDS File:
SDS
Modify Date:
2024/5/30 16:33:02

Pimobendan Properties

Melting point approximate 243℃ (dec.)
Density 1.36
storage temp. 2-8°C
solubility DMSO: soluble5mg/mL, clear (warmed)
form powder
pka 10.55±0.10(Predicted)
color white to beige
InChI 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)
InChIKey GLBJJMFZWDBELO-UHFFFAOYSA-N
SMILES C1(=O)NN=C(C2C=C3NC(C4=CC=C(OC)C=C4)=NC3=CC=2)C(C)C1
CAS DataBase Reference 74150-27-9(CAS DataBase Reference)

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P301+P310+P330
RIDADR  UN 2811 6.1 / PGIII
HS Code  2933995300
NFPA 704
0
2 0

Pimobendan price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) SML1333 Pimobendan ≥98% (HPLC) 74150-27-9 10MG ₹10825 2022-06-14 Buy
Sigma-Aldrich(India) SML1333 Pimobendan ≥98% (HPLC) 74150-27-9 50MG ₹43613.93 2022-06-14 Buy
Sigma-Aldrich(India) PHR3084 Pimobendan pharmaceutical secondary standard, certified reference material 74150-27-9 200MG ₹46460.9 2022-06-14 Buy
Product number Packaging Price Buy
SML1333 10MG ₹10825 Buy
SML1333 50MG ₹43613.93 Buy
PHR3084 200MG ₹46460.9 Buy

Pimobendan Chemical Properties,Uses,Production

Description

Pimobendan, a novel cardiotonic vasodilator, was introduced in Japan for the treatment of acute and mild to moderate chronic heart failure. It is a phosphodiesterase Ⅲ inhibitor and is able to enhance sensitization of myocardial contractile regulatory protein to calcium ions. The combination of these effects contribute to its inotropic activity. In patients with severe congestive heart failure, orally administered pimobendan improves cardiac index, stroke volume index, pulmonary wedge pressure, and systemic and pulmonary vascular resistance. Pimobendan is reported to be well tolerated and largely devoid of the proarrhythmic effects of classical phosphodiesterase Ill inhibitors. Studies also suggested that combination of the inotropic agent pimobendan with an ACE inhibitor such as enalapril may be superior to monotherapy for heart failure patients.

Chemical Properties

White Solid

Uses

Pimobendan is a cardiotonic agent. The study of the cardiotonic mechanism of Pimobendan using ventricular muscles from rabbits and guinea pigs suggests that Pimobendan acts by inhibiting phosphodiesterase III and potassium channel. The potent venodilating action of Pimobendan makes it a suitable treatment option for patients with congestive heart failure (CHF) as it also improves systemic vasoconstriction.

Definition

ChEBI: 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.

Biological Activity

Pimobendan is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.32 μM for guinea pig cardiac enzyme) that is selective for PDE3 over PDE1, PDE2, and PDE4 (IC50s = >30 μM). It is also a calcium sensitizer, decreasing the concentration of calcium required for half-maximal contractile force in isolated, skinned porcine ventricular fibers. Pimobendan increases the force of contraction in electrically-stimulated isolated guinea pig papillary muscles with an EC50 value of 6 μM, indicating positive inotropic effects. It increases survival time in dogs with congestive heart failure due to myxomatous mitral valve disease when administered in combination with angiotensin-converting enzyme inhibitors and furosemide . Formulations containing pimobendan have been used in the treatment of heart failure in dogs.

Mechanism of action

The mechanism of mild mitral regurgitation (MR) in dogs treated with Pimobendan is a dual mechanism of action, which enhances myocardial contractility by increasing calcium sensitisation of troponin C and promotes vasodilatation by inhibiting PDEIII.

Side effects

The most common side effects include gastrointestinal effects such as decreased appetite, and diarrhea. Other possible side effects include lethargy and difficulty breathing This short-acting medication should stop working within 24 hours, although effects can be longer in pets with liver or kidney disease.

in vitro

In vitro, pimobendan was O-demethylated and subsequently O-glucuronidated. The rate of metabolism of pimobendan could be maintained in this culture system for > 3 weeks. However, the relative amount of a putative N-glucuronide under in vitro conditions was lower than in vivo[1].

References

[1] S A Pahernik. “Metabolism of pimobendan in long-term human hepatocyte culture: in vivo-in vitro comparison.” Xenobiotica 25 8 (1995): 811–23.

Pimobendan Preparation Products And Raw materials

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Zenfold Sustainable Technologies (ZST) +91-9945888778 +91-9945888778 Karnataka, India 32 58 Inquiry
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Pimobendan Spectrum

4,5-dihydro-6-[2-(4-methoxyphenyl)-1h-benzimidazol-5-yl]-5-methyl-3(2h)-pyridazinone 6-(2-(4-methoxyphenyl)-1H-benzo[d]imidazol-6-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one 6-(2-(4-Methoxyphenyl)-4,5-dihydro-1H-benzimidazol-5-yl)-5-methyl-3(2H)-pyridazinone Pimobendan [inn-spanish] Pimobendane Pimobendane [inn-french] Pimobendanum PiMobendan(VetMedin) 4,5-Dihydro-6-[2-(4-Methoxyphenyl)-1H-benziMidazol-6-yl]-5-Methyl- 3(2H)-pyridazinone Acardi rac PiMobendan PiMobendan EP 6-[2-(4-Methoxy-phenyl)-1H-benzoiMidazol-5-yl]-5-Methyl-4,5-dihydro-2H-pyridazin-3-one 6-(2-(4-Methoxyphenyl)-1H-benzo[d]iMidazol-5-yl)-5-Methyl-4,5-dihydropyridazin-3(2H)-one PIMOBENDAN 3(2H)-Pyridazinone,4,5-dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-5-methyl- 4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-y1]-5-methyl-3(2H)-pyridazinone PIMOBENDANE HCL Pimobendam 3(2H)-Pyridazinone, 4,5-dihydro-6-2-(4-methoxyphenyl)-1H-benzimidazol-5-yl-5-methyl- 3(2H)-Pyridazinone, 4,5-dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-yl]-5-methyl- (9CI) dl-Pimobendan Racemic pimobendan UD-CG 115 UD-CG 115BS VETMEDIN; ACARDI; PIMOBENDANE 2-(2-Methyl-1-oxopropyl)isoindole-1,3-dione Pimobendan CRS Pimobendan for system suitability CRS 6-[2-(4-Methoxyphenyl)-1H-benzimidazol-6-yl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone Pimobendan USP/EP/BP Pimobendan 13CD3Q: What is Pimobendan 13CD3 Q: What is the CAS Number of Pimobendan 13CD3 Pimobendan D3Q: What is Pimobendan D3 Q: What is the CAS Number of Pimobendan D3 Pimobendan-D4 Pimobendan (1569315) (5RS)-6-[2-(4-Methoxyphenyl)-1H-benzimidazol-5-yl]-5- methyl-4,5-dihydropyridazin-3(2H)-one VetMedin Pimobendan/UD-CG115 74150-27-9 7415-27-9 C19H18N4O2 Aromatics Heterocycles Inhibitors Intermediates & Fine Chemicals Pharmaceuticals Inhibitor Acardi, pimobendane API 74150-27-9