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133040-01-4

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133040-01-4 Usage

Description

Teveten was launched in Germany for the treatment of hypertension. There are several ways in which it has been prepared, the shortest of which is four steps; beginning with displacement of 2-butyl-4-chloroimidazole-5-carboxaldehyde with methyl 4-(bromomethyl)benzoate. Teveten is an angiotensin Ⅱ antagonist selective for the AT, subtype receptor. It is a potent, highly selective, competitve antagonist with no agonist activity. Duration of action is similar to Enalapril (greater than 12 hr) but Teveten had a faster onset. While it is orally active, it rapidly dissociates from the receptor. This is contrary to its prolonged duration of action, which presumably results from slow removal from compartments within tissue, cells or matrix around the AT, receptor. It is not bound by BSA.

Chemical Properties

Light-Yellow Solid

Originator

SmithKline Beecham (UK)

Uses

Different sources of media describe the Uses of 133040-01-4 differently. You can refer to the following data:
1. Prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Antihypertensive
2. Eprosartan (E590100) impurity.
3. Eprosartan is a prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Eprosartan is an antihypertensive.

Definition

ChEBI: A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.

Brand name

Teveten

Clinical Use

Angiotensin-II antagonistHypertension

Drug interactions

Potentially hazardous interactions with other drugs Anaesthetics: enhanced hypotensive effect.Analgesics: antagonism of hypotensive effect and increased risk of renal impairment with NSAIDs; hyperkalaemia with ketorolac and other NSAIDs.Antihypertensives: increased risk of hyperkalaemia hypotension and renal impairment with ACE inhibitors and aliskiren.Ciclosporin: increased risk of hyperkalaemia and nephrotoxicity.Diuretics: enhanced hypotensive effect; hyperkalaemia with potassium-sparing diuretics.Epoetin: increased risk of hyperkalaemia; antagonism of hypotensive effect.Lithium: reduced excretion, possibility of enhanced lithium toxicity.Potassium salts: increased risk of hyperkalaemia.Tacrolimus: increased risk of hyperkalaemia and nephrotoxicity.

Metabolism

Following oral and intravenous dosing with [14C] eprosartan in human subjects, eprosartan was the only drug-related compound found in the plasma and faeces. In the urine, approximately 20% of the radioactivity excreted was an acyl glucuronide of eprosartan with the remaining 80% being unchanged eprosartanEprosartan is eliminated by both biliary and renal excretion. Following intravenous [14C] eprosartan, about 61% of radioactivity is recovered in the faeces and about 37% in the urine. Following an oral dose of [14C] eprosartan, about 90% of radioactivity is recovered in the faeces and about 7% in the urine.

Check Digit Verification of cas no

The CAS Registry Mumber 133040-01-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,3,0,4 and 0 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 133040-01:
(8*1)+(7*3)+(6*3)+(5*0)+(4*4)+(3*0)+(2*0)+(1*1)=64
64 % 10 = 4
So 133040-01-4 is a valid CAS Registry Number.
InChI:InChI=1/C23H24N2O4S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29)/b18-12+

133040-01-4SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 15, 2017

Revision Date: Aug 15, 2017

1.Identification

1.1 GHS Product identifier

Product name eprosartan

1.2 Other means of identification

Product number -
Other names 4-[[2-butyl-5-[(E)-2-carboxy-3-thiophen-2-ylprop-1-enyl]imidazol-1-yl]methyl]benzoic acid

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:133040-01-4 SDS

133040-01-4Related news

Enhanced dissolution/caco-2 permeability, pharmacokinetic and pharmacodynamic performance of re-dispersible EPROSARTAN (cas 133040-01-4) mesylate nanopowder09/10/2019

Eprosartan mesylate is an angiotensin receptor blocker which suffers from extremely poor bioavailability owing to its poor solubility and poor permeability. The rationale of the present work was to design the drug delivery system capable of overcoming these constraints. Nanoformulation of eprosa...detailed

Risk assessment and QbD based optimization of an EPROSARTAN (cas 133040-01-4) mesylate nanosuspension: In-vitro characterization, PAMPA and in-vivo assessment09/08/2019

Quality by design (QbD) principles were implemented to understand the product and process variables of sonoprecipitation technique, for preparation of eprosartan mesylate (EM) nanosuspension. Quality risk management approach was utilized to identify and assess high-risk attributes affecting crit...detailed

Original articleEffectiveness of EPROSARTAN (cas 133040-01-4) in diabetic hypertensive patients09/07/2019

BackgroundThe aim of this study was to compare the effectiveness and safety of eprosartan in reducing blood pressure in a group of diabetic patients and a group of non-diabetic patients in a primary care setting.detailed

Pulmonary, gastrointestinal and urogenital pharmacologyAmeliorative effect of EPROSARTAN (cas 133040-01-4) on high-fat diet/streptozotocin-induced early diabetic nephropathy in rats09/06/2019

Diabetic nephropathy becomes the single most frequent cause of end-stage renal disease. The present study aimed therefore to investigate possible protective effect of eprosartan, an angiotensin II type 1 receptor blocker, on high-fat diet/streptozotocin-induced early diabetic nephropathy in rats...detailed

Original articleFormulation and characterization of novel soft nanovesicles for enhanced transdermal delivery of EPROSARTAN (cas 133040-01-4) mesylate09/05/2019

The objective of the present work was to formulate, optimize and evaluate the potential of novel soft nanovesicles i.e. nano-transfersomes, containing eprosartan mesylate (EM) for transdermal delivery. Nano-transfersomes of EM were developed using Phospholipon 90G, Span 80 (SP) and sodium deoxyc...detailed

Spectroscopic and molecular docking studies of the binding of the angiotensin II receptor blockers (ARBs) azilsartan, EPROSARTAN (cas 133040-01-4) and olmesartan to bovine serum albumin09/04/2019

Angiotensin receptor blockers (ARBs) represent a group of widely used therapeutic agents for the effective control of hypertension and other cardiovascular problems. Herein, the interactions of three important members of the ARBs (azilsartan, eprosartan and olmesartan) with bovine serum albumin ...detailed

EPROSARTAN (cas 133040-01-4) mesylate loaded bilosomes as potential nano-carriers against diabetic nephropathy in streptozotocin-induced diabetic rats09/03/2019

The objective of the present study was to formulate eprosartan mesylate loaded nano-bilosomes and investigates its potential for controlling streptozotocin induced diabetes nephropathy in Wistar rats. The eprosartan mesylate loaded nano-bilosomes comprising of various ratios of soybean phosphati...detailed

Original research articleOATP and MRP2-mediated hepatic uptake and biliary excretion of EPROSARTAN (cas 133040-01-4) in rat and human09/02/2019

BackgroundEprosartan is an angiotensin II receptor antagonist, used in the treatment of hypertension and heart failure in clinical patients. The objective of this study was to clarify the mechanism underlying hepatic uptake and biliary excretion of eprosartan in rats and humans.detailed

133040-01-4Relevant articles and documents

1-(Carboxybenzyl)imidazole-5-acrylic Acids: Potent and Selective Angiotensin II Receptor Antagonists

Weinstock, Joseph,Keenan, Richard M.,Samanen, James,Hempel, Judith,Finkelstein, Joseph A.,et al.

, p. 1514 - 1517 (1991)

-

COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING SALT SENSITIVITY OF BLOOD PRESSURE

-

, (2015/02/05)

To characterize the urinary exosome miRNome, microarrays were used to identify the miRNA spectrum present within urinary exosomes from ten individuals that were previously classified for their salt sensitivity status. The present application discloses distinct patterns of selected exosomal miRNA expression that were different between salt-sensitive (SS), salt-resistant (SR), and inverse salt-sensitive (ISS) individuals. These miRNAs can be useful as biomarkers either individually or as panels comprising multiple miRNAs. The present invention provides compositions and methods for identifying, diagnosing, monitoring, and treating subjects with salt sensitivity of blood pressure. The applications discloses panels of miRNAs useful for comparing profiles, and in some cases one or more of the miRNAs in a panel can be used. The miRNAs useful for distinguishing SS and SR or ISS and SR subjects. One or more of the 45 miRNAs can be used. Some of the miRNAs have not been previously reported to be circulating. See those miRNAs with asterisks in FIG. 1 and below. The present invention encompasses the use of one or more of these markers for identifying and diagnosing SR, SS, and ISS subjects.

AN IMPROVED PROCESS FOR THE PREPARATION OF PURE EPROSARTANAND ITS PHARMACEUTICAL ACCEPTABLE SALTS

-

Page/Page column 7, (2011/05/11)

The present invention relates to an improved process for preparation of pure Eprosartan and its pharmaceutical acceptable salts comprising the steps of: a) treating the Eprosartan with hydrochloric acid; b) suspending the resulted Eprosartan hydrochloride

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