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    Lacidipine (GX-1048, GR-43659X, SN-305, Lacipil, Motens)
    Lacidipine (GX-1048, GR-43659X, SN-305, Lacipil, Motens)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1199
    CAS #: 103890-78-4Purity ≥98%

    Description: Lacidipine (GX-1048, GR-43659X, SN-305; GX1048, GR43659X, SN305; Caldine, Lacimen, Lacipil, Midotens, Motens) is a potent and 3rd-generation L-type CCB (calcium channel blocker) that has been approved in 1990s for treating high blood pressure. 

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

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    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


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    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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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