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product name Manidipine


Description: Manidipine is a calcium channel blocker that is used clinically as an antihypertensive agent. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cell. Manidipine is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists. 

References: Proc Natl Acad Sci U S A. 1992;89(9):4071-5; Cancer Res. 1992;52(5):1369-71.



Molecular Weight (MW)

610.7 
Formula

C35H38N4O6 
CAS No.

89226-50-6 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 122 mg/mL (199.8 mM) 
Water: <1 mg/mL
Ethanol: 3 mg/mL (4.9 mM) 
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19403712

In Vitro

In vitro activity: Manidipine, a Ca(2+)-channel blocker, at concentrations that lower elevated blood pressure, modulates the transcription rates of cytokine genes in the mesangial cells of humans that had been stimulated with platelet-derived growth factor BB isomer. Manidipine inhibits the ET-1-induced [Ca2+]i increase by reducing both the transient and sustained Ca2+ increments in A7r5 cells and glomerular mesangial cells (MCs). Manidipine (10(-5) mol/L) potentiates ET-1-induced c-fos and c-jun expression in A7r5 cells. Manidipine is a potent inhibitor for ET-1-induced [Ca2+]i signaling and that Manidipine has multiple effects on ET-1-induced signaling, including potentiating the immediate-early gene response.


Kinase Assay:


Cell Assay

In Vivo Manidipine reduces systolic blood pressure with a slight sympathetic reflex increase in heart rate, and increases plasma nitrite/nitrates in perfused rat heart from ischemia-reperfusion damage. Manidipine combined with Simvastatin reduces creatine kinase, lactate dehydrogenase and tumor necrosis factor-alpha, and enhancement of 6-keto-PGF(1alpha) during reperfusion. Manidipine hydrochloride prevents isoproterenol-induced left ventricular hypertrophy and expression of mRNA of ANP, collagen types I and type III, and fibronectin in rats with isoproterenol-induced cardiac hypertrophy. Manidipine HCl increases renal blood flow (RBF) by dilating the afferent arterioles and improves glomerular hypertension by dilating the efferent arterioles in hypertensive rats. 
Animal model  
Formulation & Dosage  
References Proc Natl Acad Sci U S A. 1992 May 1;89(9):4071-5; Eur J Pharmacol. 2008 Jun 10;587(1-3):224-30; Cancer Res. 1992 Mar 1;52(5):1369-71. 

GSK2656157

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Author: Sodium channel

Share this post on:

product name Manidipine


Description: Manidipine is a calcium channel blocker that is used clinically as an antihypertensive agent. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cell. Manidipine is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists. 

References: Proc Natl Acad Sci U S A. 1992;89(9):4071-5; Cancer Res. 1992;52(5):1369-71.



Molecular Weight (MW)

610.7 
Formula

C35H38N4O6 
CAS No.

89226-50-6 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 122 mg/mL (199.8 mM) 
Water: <1 mg/mL
Ethanol: 3 mg/mL (4.9 mM) 
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19403712

In Vitro

In vitro activity: Manidipine, a Ca(2+)-channel blocker, at concentrations that lower elevated blood pressure, modulates the transcription rates of cytokine genes in the mesangial cells of humans that had been stimulated with platelet-derived growth factor BB isomer. Manidipine inhibits the ET-1-induced [Ca2+]i increase by reducing both the transient and sustained Ca2+ increments in A7r5 cells and glomerular mesangial cells (MCs). Manidipine (10(-5) mol/L) potentiates ET-1-induced c-fos and c-jun expression in A7r5 cells. Manidipine is a potent inhibitor for ET-1-induced [Ca2+]i signaling and that Manidipine has multiple effects on ET-1-induced signaling, including potentiating the immediate-early gene response.


Kinase Assay:


Cell Assay

In Vivo Manidipine reduces systolic blood pressure with a slight sympathetic reflex increase in heart rate, and increases plasma nitrite/nitrates in perfused rat heart from ischemia-reperfusion damage. Manidipine combined with Simvastatin reduces creatine kinase, lactate dehydrogenase and tumor necrosis factor-alpha, and enhancement of 6-keto-PGF(1alpha) during reperfusion. Manidipine hydrochloride prevents isoproterenol-induced left ventricular hypertrophy and expression of mRNA of ANP, collagen types I and type III, and fibronectin in rats with isoproterenol-induced cardiac hypertrophy. Manidipine HCl increases renal blood flow (RBF) by dilating the afferent arterioles and improves glomerular hypertension by dilating the efferent arterioles in hypertensive rats. 
Animal model  
Formulation & Dosage  
References Proc Natl Acad Sci U S A. 1992 May 1;89(9):4071-5; Eur J Pharmacol. 2008 Jun 10;587(1-3):224-30; Cancer Res. 1992 Mar 1;52(5):1369-71. 

GSK2656157

Share this post on:

Author: Sodium channel