Aranidipine-MPC1304-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAranidipineCat. No.: HY-U00212CAS No.: 86780-90-7Synonyms: MPC1304分式: CHNO分量: 388.37作靶点: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Please store the product under the recommended conditions inth

2、e COA.溶解性数据体外实验 DMSO : 125 mg/mL (321.86 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5749 mL 12.8743 mL 25.7486 mL5 mM 0.5150 mL 2.5749 mL 5.1497 mL10 mM 0.2575 mL 1.2874 mL 2.5749 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Aranidipine (MPC1304)

3、种钙离 (Ca2+) 通道拮抗剂，具有强持久的抗压作。IC50 & Target Ca2+ Channel 1体内研究Aranidipine (MPC-1304) is a new Ca2+ channel antagonist in spontaneously hypertensive rats. Followingoral administration of Aranidipine at doses of 3 and 10 mg/kg to spontaneously hypertensive rats (SHR),there are significant decreases in Bm

4、ax values for specific 3H(+)-PN 200-110 binding to myocardialmembranes compared to the control values. The Bmax values at 1 h (3 mg/kg), 1 and 6 h (10 mg/kg) are1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEsignificantly decreased (47.7, 48.9 and 25.8%, respectively) compared to the control value

5、s. The effect isgreatest at 1 h and decreases with time. The Bmax values at 6 h (3 mg/kg) and 12 or 24 h (10 mg/kg) afterthe oral administration of Aranidipine are not significantly different from the control values, suggesting thedisappearance of the effect of Aranidipine. The Kd values for myocard

6、ial 3H(+)-PN 200-110 binding areunaltered by oral administration of Aranidipine 1.PROTOCOLAnimal Rats 1Administration 1 Male SHR (11-15 weeks) are used. They are fasted for 16 h before the administration of drugs, and givenAranidipine (3, 10 mg/kg) orally through a gastric tube. Control animals are

7、given the vehicle. At 1-24 h afterdrug administration, the SHR are killed by bleeding from the descending aorta under light anesthesia withethyl ether, and the myocardium and brain are perfused with 0.9% saline from the aorta. Then, both tissuesare removed, and blood vessels are trimmed away. Plasma

8、 from rat blood is isolated by centrifugation, andstored at -80C until the concentration of Aranidipine is determined.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneouslyhypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6.McePdfHeightCaution: Product has not been fully validated for medical applica