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Synonyms | UD-CG 115 BS | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H18N4O2 |
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分子量 | 334.37 | CAS No. | 74150-27-9 | ||||
Solubility (25°C)* | 体外 | DMSO | 67 mg/mL (200.37 mM) | ||||
Ethanol | 5 mg/mL (14.95 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM. |
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in vitro | 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). [1] 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. [2] 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 [3] |
in vivo | 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. [4] |
キナーゼアッセイ | Phosphodiesterase isoenzyme inhibition | |
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The isoenzymes PDE I, PDE II and PDE III are isolated from left ventricular guinea pig muscle. For determination of enzyme inhibition, Pimobendan is preincubated for 5 minutes with PDE in a buffer containing 40 mM Tris HCl, 50 mM MgCl2, and 10 mM EGTA (PH 8.0). The reaction is initiated at 37 °C by adding 0.3 μM [3H]cAMP (or 2.5 μM [3H]cGMP in the case of PDE II). The concentration of PDE is such that only 10% of the substrate is hydrolyzed during the reaction, which is stopped after 20 minutes by heating to 90 °C briefly. The reaction product [3H]AMP is split to [3H]adenosine by a phosphatase from king cobra venom. [3H]adenosine is separated from unhydrolyzed [3H]cAMP by chromatography and quantified in a scintillation counter. The concentration that produces 50% inhibition of hydrolysis (IC50) is determined from concentration-response curves. | ||
動物実験 | 動物モデル | Male DBA/2 mice of viral myocarditis |
投薬量 | 0.1 or 1 mg/kg | |
投与方法 | Orally once daily |
Identification of Small-Molecule Inhibitors of Brucella Diaminopimelate Decarboxylase by Using a High-Throughput Screening Assay. [ Front Microbiol, 2020, 10:2936] | PubMed: 32038511 |
Red-COLA1: a human fibroblast reporter cell line for type I collagen transcription [ Sci Rep, 2020, 10(1):19723] | PubMed: 33184327 |
Quantifying Drug Combination Synergy along Potency and Efficacy Axes. [ Cell Syst, 2019, 8(2):97-108] | PubMed: 30797775 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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