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Aranidipine (MPC1304)

Katalog-Nr.GC34049

Aranidipin (MPC1304) (MPC1304) ist ein Antagonist des Ca2+-Kanals mit starker und lang anhaltender blutdrucksenkender Wirkung.

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Aranidipine (MPC1304) Chemische Struktur

Cas No.: 86780-90-7

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Sample solution is provided at 25 µL, 10mM.

Description of Aranidipine (MPC1304)

Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.

Aranidipine (MPC-1304) is a new Ca2+ channel antagonist in spontaneously hypertensive rats. Following oral administration of Aranidipine at doses of 3 and 10 mg/kg to spontaneously hypertensive rats (SHR), there are significant decreases in Bmax values for specific [3H](+)-PN 200-110 binding to myocardial membranes compared to the control values. The Bmax values at 1 h (3 mg/kg), 1 and 6 h (10 mg/kg) are significantly decreased (47.7, 48.9 and 25.8%, respectively) compared to the control values. The effect is greatest at 1 h and decreases with time. The Bmax values at 6 h (3 mg/kg) and 12 or 24 h (10 mg/kg) after the oral administration of Aranidipine are not significantly different from the control values, suggesting the disappearance of the effect of Aranidipine. The Kd values for myocardial [3H](+)-PN 200-110 binding are unaltered by oral administration of Aranidipine[1].

[1]. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneously hypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6.

Protocol of Aranidipine (MPC1304)

Animal experiment:

Rats[1]Male SHR (11-15 weeks) are used. They are fasted for 16 h before the administration of drugs, and given Aranidipine (3, 10 mg/kg) orally through a gastric tube. Control animals are given the vehicle. At 1-24 h after drug administration, the SHR are killed by bleeding from the descending aorta under light anesthesia with ethyl ether, and the myocardium and brain are perfused with 0.9% saline from the aorta. Then, both tissues are removed, and blood vessels are trimmed away. Plasma from rat blood is isolated by centrifugation, and stored at -80°C until the concentration of Aranidipine is determined.

References:

[1]. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneously hypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6.

Chemical Properties of Aranidipine (MPC1304)

Cas No. 86780-90-7 SDF
Canonical SMILES O=C(C1=C(C)NC(C)=C(C(OCC(C)=O)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
Formula C19H20N2O7 M.Wt 388.37
Löslichkeit DMSO : 125 mg/mL (321.86 mM) Storage Store at -20°C,unstable in solution, ready to use.
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Aranidipine (MPC1304)

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1 mg 5 mg 10 mg
1 mM 2.5749 mL 12.8743 mL 25.7486 mL
5 mM 0.515 mL 2.5749 mL 5.1497 mL
10 mM 0.2575 mL 1.2874 mL 2.5749 mL
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