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MedChemExpress - Model Manidipine dihydrochloride - 89226-75-5

Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection[1][2][3][4][5][6].

Manidipine dihydrochloride

MCE China：Manidipine dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-17403

CAS：89226-75-5

Synonyms：CV-4093

Purity：99.91%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.

In Vitro：Manidipine dihydrochloride (1 μM, 42 h) suppresses IL-6 secretion in lipoproteins-induced HUVEC[3]. Manidipine dihydrochloride (1 μM, 16 h) suppresses IL-6 secretion in 10 ng/mL IL-1, 10 ng/mL IFN-γ, and 25 ng/mL TNFα treated THP-I [3]. Manidipine dihydrochloride (20 mg/mL, 48/20 h) inhibits propagation/genome replication of SFTSV (a negative-strand RNA virus) in SW13 cells[4]. Manidipine dihydrochloride (20 mg/mL, 48 h) interferes SFTSV N-induced inclusion body formation in Huh-7 cells[4].

In Vivo：Manidipine dihydrochloride (10 mg/kg, i.p., b.i.d. at day 4, day 5) prolongs survival in SFTSV-infected mice[4]. Manidipine dihydrochloride (25 mg/kg, i.p., b.i.d. for 2 d, then daily for 19 d) protects mice from JEV infection[5]. Manidipine dihydrochloride (3 mg/kg, i.g., once per day, 7 d) prevents isoproterenol-induced left ventricular hypertrophy in rats[7].

IC50 & Target：T-type calcium channel

References：

[1]. Roca-Cusachs A, et al. Antihypertensive effect of manidipine. Drugs. Drugs. 2005，65，11-19. [Content Brief]

[2]. Cavalieri L,, et al. Metabolic effects of manidipine. Am J Cardiovasc Drugs. 2009，9，3. [Content Brief]

[3]. Franco Bernini, et al. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Pharmacol Res. 2010，62，3. [Content Brief]

[4]. Urata S, et al. Calcium Influx Regulates the Replication of Several Negative-Strand RNA Viruses Including Severe Fever with Thrombocytopenia Syndrome Virus. J Virol. 2023，97，3. [Content Brief]

[5]. Wang S, et al. Screening of FDA-Approved Drugs for Inhibitors of Japanese Encephalitis Virus Infection. J Virol. 2017，91，21. [Content Brief]

[6]. Tohse N, et al. Voltage-dependent modulation of L-type Ca2+ current by manidipine in guinea-pig heart cells. Eur J Pharmacol. 1993，249(2):231-3. [Content Brief]

[7]. Yoshiyama M, et al. Effect of manidipine hydrochloride, a calcium antagonist, on isoproterenol-induced left ventricular hypertrophy. Pharmacol Res. 2010Jpn Circ J. 1998，62(1):47-52. [Content Brief]

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