Lacidipine Chemical Properties

Melting point:

174-175°C

Boiling point:

558.4±50.0 °C(Predicted)

Density 

1.127±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

3.00±0.70(Predicted)

color 

white to beige

Merck 

14,5331

InChIKey

GKQPCPXONLDCMU-CCEZHUSRSA-N

CAS DataBase Reference

103890-78-4(CAS DataBase Reference)

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

3

RTECS 

US7970200

Toxicity

mouse,LD50,intraperitoneal,80200ug/kg (80.2mg/kg),SKIN AND APPENDAGES (SKIN): HAIR: OTHERSENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYEBEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY),Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 22, Pg. 335, 1994.

MSDS

• Language:English Provider:Lacidipine

Lacidipine Usage And Synthesis

Description

Lacidipine is a new second-generation dihydropyridine calcium antagonist introduced as a once a day treatment for mild to moderate hypertension. It is reported to have high selectivity for vascular smooth muscle and also a long duration of action. The use of lacidipine as an antiatherosclerotic agent is currently under investigation.

Description

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.

Chemical Properties

White-to-Off-White Crystalline Solid

Originator

Glaxo (United Kingdom)

Uses

A dihydropyridine calcium channel blocker. Antihypertensive.

Uses

antihypertensive;dihydropyridinr calcium channel blocker

Definition

ChEBI: Lacidipine is a cinnamate ester and a tert-butyl ester.

brand name

Lacipil; Lacirex; Viapres

Biochem/physiol Actions

Lacidipine is a long-acting calcium antagonist that is used in the management of hypertension. Lacidipine is a L-type Ca(2+) channel blocker belonging to 1,4-dihydropyridine class. Also, Lacidipine inhibits ryanodine receptors on the ER membrane that enhances folding, trafficking and lysosomal activity of ERAD (ER-associated degradation) misfolded lysosomal glucocerebrosidase (GS).

Lacidipine(103890-78-4)Related Product Information

• Phenyl salicylate
• Ethoxyquin
• DIETHOXYMETHANE
• Diphenyl ether
• PHENYL VALERATE
• Fentin hydroxide
• Ethoxyamine hydrochloride
• PHENYL RESIN
• Phenylacetic acid
• Oxygen
• cis Lacidipine
• trans Lacidipine-d10,LACIDIPINE-D10
• Dehydro Lacidipine
• 2,6-DIMETHYL-3,5-PYRIDINEDICARBOXYLIC ACID
• Lacidipine
• LACIDIPINE INTERMEDIATE:4-(2-BROMOPHENYL)-1,4-DIHYDRO-2,6-DIMETHYL-3,5-PYRIDINEDICARBOXYLIC ACID DIETHYL ESTER
• 4-(2-bromophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid diethyl ester (intermediate of lacidipine)
• LACIDIPINE IMPURITY STANDARD