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103890-78-4

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103890-78-4 Usage

Description

Different sources of media describe the Description of 103890-78-4 differently. You can refer to the following data:
1. 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.
2. 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

Different sources of media describe the Uses of 103890-78-4 differently. You can refer to the following data:
1. A dihydropyridine calcium channel blocker. Antihypertensive.
2. A dihydropyridine calcium channel blocker. Antihypertensive
3. antihypertensive;dihydropyridinr calcium channel blocker

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).

Clinical Use

#N/A

Drug interactions

Potentially hazardous interactions with other drugs Aminophylline and theophylline: possibly increased aminophylline and theophylline concentration. Anaesthetics: enhanced hypotensive effect. Antibacterials: metabolism possibly inhibited by clarithromycin, erythromycin and telithromycin. Antidepressants: enhanced hypotensive effect with MAOIs. Antiepileptics: effect possibly reduced by carbamazepine, barbiturates, phenytoin and primidone. Antifungals: metabolism possibly inhibited by itraconazole and ketoconazole; negative inotropic effect possibly increased with itraconazole. Antihypertensives: enhanced hypotensive effect, increased risk of first dose hypotensive effect of postsynaptic alpha-blockers. Antivirals: concentration possibly increased by ritonavir. Ciclosporin: 10 kidney transplant patients on ciclosporin, prednisone and azathioprine were given 4 mg lacidipine daily. A very small increase in the trough serum levels (+6%) and AUC (+14%) of the ciclosporin occurred. Grapefruit juice: concentration increased - avoid concomitant use

Metabolism

Lacidipine undergoes extensive first-pass metabolism in the liver. The drug is eliminated primarily by hepatic metabolism (involving cytochrome P450 CYP3A4). The principal metabolites possess little, if any, pharmacodynamic activity. Approximately 70% of the administered dose is eliminated as metabolites in the faeces and the remainder as metabolites in the urine.

Check Digit Verification of cas no

The CAS Registry Mumber 103890-78-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,3,8,9 and 0 respectively; the second part has 2 digits, 7 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 103890-78:
(8*1)+(7*0)+(6*3)+(5*8)+(4*9)+(3*0)+(2*7)+(1*8)=124
124 % 10 = 4
So 103890-78-4 is a valid CAS Registry Number.
InChI:InChI=1/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+

103890-78-4 Well-known Company Product Price

  • Brand
  • (Code)Product description
  • CAS number
  • Packaging
  • Price
  • Detail
  • TCI America

  • (L0276)  Lacidipine  >98.0%(HPLC)(N)

  • 103890-78-4

  • 200mg

  • 790.00CNY

  • Detail
  • TCI America

  • (L0276)  Lacidipine  >98.0%(HPLC)(N)

  • 103890-78-4

  • 1g

  • 2,590.00CNY

  • Detail
  • Sigma

  • (SML0946)  Lacidipine  ≥98% (HPLC)

  • 103890-78-4

  • SML0946-10MG

  • 734.76CNY

  • Detail
  • Sigma

  • (SML0946)  Lacidipine  ≥98% (HPLC)

  • 103890-78-4

  • SML0946-50MG

  • 2,975.31CNY

  • Detail

103890-78-4SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name diethyl 2,6-dimethyl-4-[2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate

1.2 Other means of identification

Product number -
Other names Motens

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:103890-78-4 SDS

103890-78-4Related news

Formulation and optimization of Lacidipine (cas 103890-78-4) loaded niosomal gel for transdermal delivery: In-vitro characterization and in-vivo activity07/25/2019

The aim of the present research work is to formulate lacidipine (LAC) loaded niosomes formulation for the management of hypertension by thin film hydration technique. The developed formulations were statistically optimized by four factors, three levels Box–Behnken design and were evaluated for ...detailed

Virtual population pharmacokinetic using physiologically based pharmacokinetic model for evaluating bioequivalence of oral Lacidipine (cas 103890-78-4) formulations in dogs07/24/2019

The aim of the present study was to investigate virtual population pharmacokinetic using physiologically based pharmacokinetic (PBPK) model for evaluating bioequivalence of oral lacidipine formulations in dogs. The dissolution behaviors of three lacidipine formulations including one commercial p...detailed

Rapidly dissolving Lacidipine (cas 103890-78-4) nanoparticle strips for transbuccal administration07/22/2019

The purpose of this study was to prepare fast-dissolving film strips containing lacidipine (LCDP) nanoparticles for transbuccal administration. Nanoparticles were prepared using the solvent-antisolvent sonoprecipitation technique. The influence of different antisolvent phase stabilizers on parti...detailed

Lacidipine (cas 103890-78-4) attenuates TNF-α-induced cardiomyocyte apoptosis07/20/2019

This study was designed to investigate whether lacidipine elicited a protective role on cardiomyocyte against apoptosis induced by TNF-α. Neonatal rat cardiomyocytes were randomly assigned into different groups. TUNEL staining was utilized to detect apoptosis, and caspase-3 and caspse-12 were d...detailed

Synergetic effect of nucleation and crystal growth inhibitor on in vitro-in vivo performance of supersaturable Lacidipine (cas 103890-78-4) solid dispersion07/21/2019

Limited supersaturation maintaining duration is the main challenge for amorphous solid dispersion design. Nucleation or crystal growth inhibitors may function in different ways but the combination use of nucleation and crystal growth inhibitors in supersaturated system is rarely explored. Thus, ...detailed

103890-78-4Relevant articles and documents

METHODS FOR TREATING CHRONIC FATIGUE SYNDROME AND MYALGIC ENCEPHALOMYELITIS

-

, (2021/03/13)

In one aspect the invention relates to a method of treatment selected from the group consisting of: (a) treating a symptom such as pain in a subject identified or diagnosed as having Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS); (b) treating a symptom such as pain in a subject having dysfunctional TRPM3 ion channel activity; (c) restoring NK cell function in a subject having dysfunctional TRPM3 ion channel activity; and (d) restoring calcium homeostasis in a subject having dysfunctional TRPM3 ion channel activity. The method comprises the step of administering to the subject a therapeutically effective amount of at least one therapeutic compound selected from the group consisting of: (i) an opioid receptor antagonist; (ii) an opioid antagonist; and (iii) a therapeutic compound that restores TRPM3 ion channel activity. In some embodiments the therapeutic compound is naltrexone hydrochloride.

THERAPY FOR COMPLICATIONS OF DIABETES

-

, (2009/07/02)

A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.

PROCESS FOR PREPARING LACIDIPINE

-

Page/Page column 6, (2010/11/25)

A process for preparing lacidipine, comprising reacting a t-butoxy carbonyl methyl aryl phosphonium halide with o-phthalaldehyde, and further reacting a product comprising (E)-3-(2-formylphenyl)-2-propenoic acid, 1,1-dimethyl ethyl ester, without isolation, with ethyl-3-amino crotonate.

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