Lacidipine

Lacidipine is a dihydropyridine L-type calcium channel blocker. It induces relaxation of isolated rat aorta and inhibits calcium-induced contraction of rabbit ear artery (pA2 = 9.4). It also induces relaxation of calcium-induced contractions in isolated rat colon and bladder and guinea pig trachea (IC50s = 6.7, 6, and 7.8 nM, respectively). Lacidipine induces negative inotropy in isolated guinea pig ventricular strips (IC50 = 110 nM). It reduces mean blood pressure in spontaneously hypertensive rats (ED25 = 0.35 mg/kg) and in renal hypertensive dogs (ED25 = 0.22 mg/kg) with a transient increase in heart rate. Lacidipine inhibits copper-induced oxidation of isolated human LDL when used at concentrations of 1 and 5 µM. It reduces the extension of aortic atheromatous lesions and decreases renal injury in ApoE-/- mice in a model of Western diet-induced atherosclerosis.Formal Name: 4-[2-[(1E)-3-(1,1-dimethylethoxy)-3-oxo-1-propen-1-yl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid, 3,5-diethyl ester. CAS Number: 103890-78-4. Synonyms: GX 1048, GR 43659X. Molecular Formula: C26H33NO6. Formula Weight: 455.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25mg/mL, DMF:PBS (pH 7.2) (1:3): 0.25mg/mL, DMSO: 20mg/mL, Ethanol: 5mg/ml. lambdamax: 240, 284, 368 nm. SMILES: CC1=C(C(OCC)=O)C(C2=C(/C=C/C(OC(C)(C)C)=O)C=CC=C2)C(C(OCC)=O)=C(C)N1. InChi Code: InChI=1S/C26H33NO6/c1-8-31-24(29)21-16(3)27-17(4)22(25(30)32-9-2)23(21)19-13-11-10-12-18(19)14-15-20(28)33-26(5,6)7/h10-15,23,27H,8-9H2,1-7H3/b15-14+. InChi Key: GKQPCPXONLDCMU-CCEZHUSRSA-N.