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100427-26-7

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100427-26-7 Usage

Description

Lerdip was launched in the Netherlands for hypertension. It is prepared in four steps, the last of which is a Hantsch reaction of 1-[(3,3-diphenyl)-N-methylpropylamino]- 2-methyl-2-propyl-2-(3-nitrobenzylidene)acetoacetate with methyl 3-aminocrotonate. This compound was designed to be very lipophilic which imparts the drug with a gradual onset and a long duration of action as a result of prolonged exposure to receptors by partitioning into membranes. It is an antagonist of L-type calcium channels with no activity in smooth muscle cells, is tissue selective, lacks any myocardial contractility impairment, has no neuroendocrine activation, and has negligible affinity for neurotransmitter receptors such as α1- and α2-adrenergic receptors. While sold as a racemate, the calcium channel activity is found in the (S)- isomer with the (R)-isomer being 2-orders of magnitude less active. It has an increased cardiac contractility index which is much more than Nitrendipine or nifedipine. The good selectivity causes a reduction in blood pressure with no negative inotropic effects.

Originator

Recordati (Italy)

Uses

Antihypertensive compound; calcium channel blocker.

Brand name

Cardiovasc (Recor dati, Italy); Carmen (Recordati, Italy); Corifeo (Recordati, Italy); Lercadip (Recordati, Italy); Lercan (Recordati, Italy); Lercapin (Recordati, Italy); Lercaton (Recordati, Italy); Lerkamen (Recordati, Italy); Lerzam (Recordati, Italy); Renovia (Recordati, Italy); Vasodip (Recordati, Italy); Zandip (Recordati, Italy); Zanicor (Recordati, Italy).

Check Digit Verification of cas no

The CAS Registry Mumber 100427-26-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,0,4,2 and 7 respectively; the second part has 2 digits, 2 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 100427-26:
(8*1)+(7*0)+(6*0)+(5*4)+(4*2)+(3*7)+(2*2)+(1*6)=67
67 % 10 = 7
So 100427-26-7 is a valid CAS Registry Number.
InChI:InChI=1/C36H41N3O6/c1-24-31(34(40)44-6)33(28-18-13-19-29(22-28)39(42)43)32(25(2)37-24)35(41)45-36(3,4)23-38(5)21-20-30(26-14-9-7-10-15-26)27-16-11-8-12-17-27/h7-19,22,30,33,37H,20-21,23H2,1-6H3

100427-26-7SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name 5-O-[1-[3,3-diphenylpropyl(methyl)amino]-2-methylpropan-2-yl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

1.2 Other means of identification

Product number -
Other names UNII-V7XTJ4R0BH

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:100427-26-7 SDS

100427-26-7Related news

Evaluation of the Efficacy and Safety of the Lercanidipine (cas 100427-26-7)/Valsartan Combination in Korean Patients With Essential Hypertension Not Adequately Controlled With Lercanidipine (cas 100427-26-7) Monotherapy: A Randomized, Multicenter, Parallel Design, Phase III Clinical Trial07/31/2019

PurposeThe objective of this study was to evaluate the efficacy and safety of the lercanidipine/valsartan combination compared with lercanidipine monotherapy in patients with hypertension.detailed

Neuroprotective effect of Lercanidipine (cas 100427-26-7) in middle cerebral artery occlusion model of stroke in rats07/29/2019

Oxidative stress, inflammation and apoptotic neuronal cell death are cardinal mechanisms involved in the cascade of acute ischemic stroke. Lercanidipine apart from calcium channel blocking activity possesses anti-oxidant, anti-inflammatory and anti-apoptotic properties. In the present study, we ...detailed

100427-26-7Relevant articles and documents

THERAPY FOR COMPLICATIONS OF DIABETES

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, (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.

Method for treating resistant hypertension

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, (2008/06/13)

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Solid lercanidipine free base

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Page/Page column 8, (2008/06/13)

The invention provides substantially pure lercanidipine free base, having a purity of at least 95%, preferably at least 97%, more preferably at least 99%, and still more preferably at least 99.5%. The lercanidipine free base of the present invention is fo

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