Lacidipine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lacidipine (Lacipil, Motens) 是一种 L 型钙通道阻滞剂。

Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker.Lacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depl.(In Vitro):Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner.Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway.(In Vivo):Lacidipine (0.3, 1.0, 3.0 mg/kg; p.o.; single daily for 10 weeks) shows anti-atherogenic effects in the apoE-deficient mouse, and reduces plasma endothelin concentrations.

Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner.Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway. Cell Proliferation Assay Cell Line:HKC cells Concentration:0.01-100 μM Incubation Time:24 h Result:Exhibited anti-proliferative activity in a concentration-dependent manner.Apoptosis Analysis Cell Line:HKC cells (renal ischemia reperfusion (I/R) model) Concentration:1, 10 μM Incubation Time:24 h Result:AA-induced HKC cells apoptosis, with proportion of early apoptotic cells of 1.47% and 0.30% for 1 and 10 μM dosage, respectively.Western Blot Analysis Cell Line:HKC cells (renal ischemia reperfusion (I/R) model)Concentration:1, 10 μM Incubation Time:24 h (pretreat) Result:Decreased the expression of cyt c of injured cells following ATP depletion and recovery.Significantly increased the expression of the Bcl-2 protein, but decreased the Bax protein.

Lacidipine (0.3, 1.0, 3.0 mg/kg; p.o.; single daily for 10 weeks) shows anti-atherogenic effects in the apoE-deficient mouse, and reduces plasma endothelin concentrations. Animal Model:Female C57BL/6 mice (Homozygous; apoE-deficient; atherosclerosis model).Dosage:0.3, 1.0, 3.0 mg/kg Administration:Oral gavage; single daily for 10 weeks.Result:Induced a significant dose-dependent decrease in plasma endothelin levels.Significantly reduced the mean lesion area in a dose-related manner by 10, 17 and 53% for 0.3, 1.0, 3.0 mg/kg, respectively.

Lacidipine | Lacipil | Lacimen | Motens | GR 43659 X

GPCR/G Protein

Calcium Channel

Calcium Channel

Cardiovascular Disease

——

103890-78-4

455.54

C26H33NO6

>98% (HPLC)

Ethanol: 22 mg/mL (48.29 mM); DMSO: 91 mg/mL (199.76 mM)

O=C(C1=C(C)NC(C)=C(C(OCC)=O)C1C2=CC=CC=C2/C=C/C(OC(C)(C)C)=O)OCC

diethyl (E)-4-(2-(3-(tert-butoxy)-3-oxoprop-1-en-1-yl)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

(-20℃)

With Ice Pack

≥ 2 years