For research use only.
Catalog No.S1994 Synonyms: GX-1048, GR-43659X, SN-305
CAS No. 103890-78-4
Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
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Choose Selective Calcium Channel Inhibitors
|Description||Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.|
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.  Lacidipine almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages. 
|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.  Lacidipine (1 and 3 mg/kg) also effectively increases calcium concentrations significantly in ovariectomized rats.  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. |
-  Wang F, et al. Chem Biol,?011, 18(6), 766-776.
-  Bernini F, et al. Br J Pharmacol,?997, 122(6), 1209-1215.
-  Kyselovic J, et al. Br J Pharmacol,?001, 134(7), 1516-1522.
|In vitro||DMSO||91 mg/mL (199.76 mM)|
|Ethanol||22 mg/mL (48.29 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||GX-1048, GR-43659X, SN-305|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00533858||Unknown status||Drug: lacidipine (4 mg) or losartan (50 mg)||Hypertension||Seoul National University Hospital||September 2007||Phase 4|
|NCT00328965||Completed||Drug: Lacidipine||Diabetes Mellitus Type 2|Essential Hypertension||GlaxoSmithKline||November 2004||Phase 4|
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