Pimobendan-UD-CG115-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPimobendanCat. No.: HY-B0204CAS No.: 74150-27-9Synonyms: UD-CG115分式: CHNO分量: 334.37作靶點(diǎn): Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO :

2、50 mg/mL (149.53 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.9907 mL 14.9535 mL 29.9070 mL5 mM 0.5981 mL 2.9907 mL 5.9814 mL10 mM 0.2991 mL 1.4953 mL 2.9907 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液

3、，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (8.22 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (8.22 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 M

4、aster of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.75 mg/mL (8.22 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pimobendan (UD-CG115)是PDE3 選擇性抑制劑，IC50為 320nM。IC50 & Target PDE3 1.體外研究 Pimobendan (UD-CG115) exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle withIC50 o

5、f 0.32 uM compared to the inhibition of PDE I and PDE II (IC50 30 M). In human atrial cells, 100 MPimobendan (UD-CG115) significantly increases the L-type calcium current (ICa(L) (evoked bydepolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation(EC50 )

6、 of 1.13 M. 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.體內(nèi)研究 Pimobendan (UD-CG115) shows a beneficial effect on survival in the murine model of EMC virus-inducedmyocarditis. Administration

7、of Pimobendan (UD-CG115) significantly increases the final survival rate from33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (UD-CG115) (1 mg/kg) alsosignificantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)- andinterleukin (IL)

8、-1 compared with the control group, which shows no effect on myocardial necrosis, heartweight and body weight. Pimobendan (UD-CG115) suppresses expression of the intracardiac iNOS gene ,causing reduction of intracardiac NO production 2.PROTOCOLAnimal Mice 2Administration 2 Since, in this model, most

9、 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/kgor 1 mg/kg daily for 14 days from the day of EMC virus inoculation while control mice received vehicles only.T

10、hirty mice were randomly assigned to each group 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kajimoto K, et al. Contribution of phosphodiesterase isozymes to the regulation of the L-type calcium current in human cardiacmyocytes. 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 synthasein a murine model of viral myocarditis. J Am Coll Cardiol. 1999 Apr;33(5):1400-7.McePdfHeightCaution: Product has not be