Home Transmembrane Transporters Calcium Channel inhibitor Lacidipine For research use only.

Lacidipine

Synonyms: GX-1048, GR-43659X, SN-305

Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.

Lacidipine Chemical Structure

Lacidipine Chemical Structure

CAS: 103890-78-4

Purity & Quality Control

Batch: S199401 DMSO] 91 mg/mL] false] Ethanol] 22 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

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Biological Activity

Description Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
Targets
L-type calcium channel [1]
In vitro
In vitro Lacidipine, an L-type Ca(2+) channel blocker that also inhibits [Ca(2+)](ER) efflux, enhances folding, trafficking, and activity of degradation-prone glucocerebrosidase (GC) variants. Lacidipine remodels mutated GC proteostasis by simultaneously activating a series of distinct molecular mechanisms, namely modulation of Ca(2+) homeostasis, upregulation of the ER chaperone BiP, and moderate induction of the unfolded protein response. [1] Lacidipine almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages. [2]
In Vivo
In vivo Lacidipine has non-significant effects on blood pressure but inhibits the paradoxical increases in plasma renin activity (PRA) and in renin mRNA in kidney that are found in salt-loaded stroke-prone spontaneously hypertensive rats (SHRSP). Lacidipine restores the physiological downregulation of renin production by high salt and reduces left ventricular hypertrophy and mRNA levels of atrial natriuretic factor and transforming growth factor-beta1. [3] Lacidipine (1 and 3 mg/kg) also effectively increases calcium concentrations significantly in ovariectomized rats. [4] Lacidipine, a dihydropyridine-type calcium antagonist, reduces the cardiac hypertrophy and the cardiacendothelin-1 (ET-1) gene overexpression occurring in salt-loaded stroke-prone spontaneously hypertensive rats (SL-SHRSP), an effect occurring without systolic blood pressure (SBP) change. Lacidipine exerts a dose-related inhibition of ventricle hypertrophy and preproET-1-mRNA expression in SHRSP and indicate that this effect is unrelated to SBP changes. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00533858 Unknown status Hypertension Seoul National University Hospital September 2007 Phase 4
NCT00328965 Completed Diabetes Mellitus Type 2|Essential Hypertension GlaxoSmithKline November 2004 Phase 4

Chemical lnformation & Solubility

Molecular Weight 455.54 Formula

C26H33NO6
CAS No. 103890-78-4 SDF Download Lacidipine SDF
Smiles CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2C=CC(=O)OC(C)(C)C)C(=O)OCC)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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