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Lacidipine(GX-1048,GR-43659X,SN-305,Lacipil,Motens)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lacidipine(GX-1048,GR-43659X,SN-305,Lacipil,Motens)图片
CAS NO:103890-78-4
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)455.54
FormulaC26H33NO6
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)NA
SynonymsGX-1048, GR-43659X, SN-305; GX 1048, GR 43659X, SN 305; GX1048, GR43659X, SN305; Lacipil, Motens
实验参考方法
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.

In VivoLacidipine 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 modelRats
Formulation & Dosage1 and 3 mg/kg
References

Chem Biol. 2011 Jun 24;18(6):766-76; Br J Pharmacol. 2001 Dec;134(7):1516-22.