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 team.
Why Aurigene Pharmaceutical Services?
Quick turnaround time
State-of-the-art facilities
Extensive experience in the hERG assay & GLP FOB studies
Team of expert scientists
Virtual Tour
Hyderabad R and D Center
Bangalore R and D Center
Toxicology Studies
Resources
FEBRUARY 23, 2021
Emerging Trends in Solid State Phase Peptide Synthesis
Peptides are short chains of amino acids that are linked by peptide bonds. Peptides are highly specific and offer improved toxicological profiles. Peptides are produced using one of three synthesis methods: Solid phase peptide synthesis, liquid phase pepide synthesis or a hybrid approach.Solid-phase peptide synthesis(SPPS) is one of the most commonly used techniq...
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Evolution in Pharma Industry and Demand for Integrated CDMO
The pharma industry is evolving and a demand for integrated CDMOs, which can help accelerating innovations, is part of the evolution....
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Systematic formulation design - shorten development cost & time
Project Challenge: Existing formulation (lower strength - 50 mg) was manufactured using direct compression process. This formulation posed poor powder flow and content uniformity issues during scale-up. Development of new strength 150 mg without any process issues was a challenge. Solution design: Preliminary pre-formulation, stress study and PSD impact assessmen...
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Construction of a six-membered fused N-heterocyclic ring via a new 3-component reaction: synthesis of (pyrazolo)pyrimidines/pyridinesw
2012
A conceptually new three-component reaction was developed to construct a six-membered fused N-heterocyclic ring affording (pyrazolo)pyrimidines/pyridines as potential inhibitors of PDE4. The reaction is catalyzed by triflic acid in acetic acid in the presence of aerial oxygen. ...
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Alternate end-game strategies towards Nirmatrelvir synthesis: Defining a continuous flow process for the preparation of an anti-COVID drug
2005
Scalable alternate end-game strategies for the synthesis of the anti-COVID drug molecule Nirmatrelvir (1,PF-07321332) have been described. The first involves a direct synthesis of 1 via amidation of the carboxylic acid 7 (suitably activated as a mixed anhydride with either pivaloyl chloride or T3P) with the ...
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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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Synthesis of Anti-covid Drug Nirmatrelvir Using Flow Chemistry
2005
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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