The cardiac potassium channel, hERG, is responsible for a rapid delayed rectifier current (IKr), which is primarily responsible for cardiac Action Potential (AP) repolarization. The unique structural properties of hERG make it vulnerable to interaction and inhibition by large numbers of compounds. Inhibition of IKr is the most common cause of cardiac AP prolongation by non-cardiac drugs. Prolonged AP causes prolongation of QT interval and has been associated with fatal ventricular arrhythmia, and Torsade de Pointes - which has led to a number of drug withdrawals and failures.
We conduct a Functional Observational Battery (FOB) test for the assessment of neurobehavioral changes induced by the test compound. Typically, various graded concentrations of test articles are formulated in suitable vehicles and administered to rats or mice. Studies are conducted as a single exposure regimen or as part of repeat dose toxicity studies. The pre and post-dose FOB measurements on the same day are made to evaluate the intra and intergroup comparison of effects.
Our scientists have vast experience in handling various test modules. The studies are conducted in full GLP compliance and data are reviewed by the Quality Assurance (QA) team.
Why Aurigene Safety Pharmacology Services?
Quick turnaround time
State-of-the-art facilities
Extensive experience in the hERG assay & GLP FOB studies
Team of expert scientists
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Bangalore R and D Center
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Our team of experts is dedicated to providing personalised solutions tailored to your unique needs. So, please don't hesitate to reach out to us. We look forward to hearing from you and helping you achieve your business goals.
Resources
OCTOBER 01, 2024
PROTACs: Research for a life without cancer
PROTACs: Proteolysis-targeting chimeras (PROTACs) are a rapidly evolving field with promising applications in cancer, neurodegenerative diseases, and other conditions where the regulation of protein levels is crucial. PROTACs are a novel class of small molecules designed to target specific proteins for degradation by the ubiquitin-proteasome sys...
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Advancement in personalized medicine and how the CRDMO industry is part of the solution
Personalized medicine is transforming the healthcare landscape by customizing treatment plans to individual patients’ unique genetic, clinical and environmental characteristics. These are effective and less invasive treatments for a wide range of conditions. Contract Research, Development and Manufacturing Organizations (CRDMOs) play an important role...
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Cell Line Development
We enable development of stable and high yielding recombinant Mammalian and Microbial lines. ...
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Case study: Tackling CYP 2C9 inhibition challenges
The Problem: Active compounds in a project were found to be highly potent inhibitors of CYP 2C9 The compounds selectively inhibited CYP 2C9 with IC50 values <100 nM There was no considerable inhibition of the other CYP isoforms Our Mitigation Approach: CYP 2C9 inhibition data was generated for a larger set of co...
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Synthesis of Anti-covid Drug Nirmatrelvir Using Flow Chemistry
2022
Synthesis of the anti-covid therapeutic Nirmatrelvir by using flow chemistry to enhance efficiency of amide to nitrile conversion in a functionally and Stereochemically Embellished environment. ...
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Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
2005
Mutations in MEK1/2 have been described as a resistance mechanism to BRAF/MEK inhibitor treatment. We report the discovery of a novel ATP-competitive MEK1/2 inhibitor with efficacy in wildtype (WT) and mutant MEK12 models. Starting from a HTS hit, we obtained selective, cellularly active ...
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Wang-OSO3H catalyzed green synthesis of bioactive isoindolo[2,1- a ]quinazoline-5,11–dione derivatives: An unexpected observation
2005
The sulphonic acid-functionalized Wang resin (Wang-OSO3H) was explored as a polymeric and recov- erable acidic catalyst for the synthesis of isoindolo[2,1- a ]quinazoline-5,11–dione derivatives under green conditions. Thus the Wang-OSO3H ...
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Polycyclic Aromatic Compounds: A Simple and Efficient [(n-Bu3Sn)2MO4]n Catalyzed Synthesis of Quinazolinones and Dihydroquinazolinones
2005
A novel unprecedented approach for the synthesis of various quinazolinones and dihydroquinazolinones has been using [(n-Bu3Sn)2MO4]n as a catalyst. The reaction has been screened ...
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