product name Lacidipine
Description: Lacidipine (also known as GX-1048, GR-43659X, SN-305) is a novel third-generation L-type calcium channel blocker used for treating high blood pressure. 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.
References: Chem Biol. 2011 Jun 24;18(6):766-76; Br J Pharmacol. 2001 Dec;134(7):1516-22.
455.54
Formula
C26H33NO6
CAS No.
103890-78-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 91 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 22 mg/mL (48.3 mM)
Solubility (In vivo)
Synonyms
GX-1048,GR-43659X,SN-305
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403811
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Chem Biol. 2011 Jun 24;18(6):766-76; Br J Pharmacol. 2001 Dec;134(7):1516-22. |
Related Posts
product name Lacidipine
Description: Lacidipine (also known as GX-1048, GR-43659X, SN-305) is a novel third-generation L-type calcium channel blocker used for treating high blood pressure. 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.
References: Chem Biol. 2011 Jun 24;18(6):766-76; Br J Pharmacol. 2001 Dec;134(7):1516-22.
455.54
Formula
C26H33NO6
CAS No.
103890-78-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 91 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 22 mg/mL (48.3 mM)
Solubility (In vivo)
Synonyms
GX-1048,GR-43659X,SN-305
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403811
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Chem Biol. 2011 Jun 24;18(6):766-76; Br J Pharmacol. 2001 Dec;134(7):1516-22. |