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Discovery Solutions for Small Molecules

  • In-Vitro Biology studies provide invaluable data on a compound's chances to succeed at the Preclinical phase.
  • At DiponEd CRS division, we provide solutions right from conception to delivery of targets.
  • We offer a panel of in vitro pharmacological assays that cover a broad range of targets.
  • Determination of potency of the NCE on target, selectivity screening and profiling.
  • While working closely with the customers, the team provides solutions ranging from
    • Reagent generation,
    • Screening and determination of potency
    • Assay development,
    • Characterization of binding and Kinetic parameters
    • Assay validation and

IN-VITRO BIOLOGY SERVICES

  • Cell based assays
    • Inhibition assays
    • Binding assays
    • Uptake inhibition assays (Glucose, Nicotinic acid)
    • ELISA
    • Transporter assays (SGLT and SMCT)
    • Cytotoxicity assays
  • Enzyme assays
    • Standardization and Validation
    • Evaluation of concentration dependent curves
    • Determination of EC50, EC90 and IC50

IN VITRO BIOLOGY

  • Enzyme Kinetics (drug/new chemical entity)
    • Determination of reversible and irreversible inhibition
    • Determination of Competitive, Non-Competitive, Uncompetitive and Mixed inhibition
    • Determination of Slow and Fast binding, Slow and Fast relieving
    • Determination of Kon, Koff and t1/2
    • Determination Kinetic Rate Index (KRI)
  • Other In-Vitro assays
    • GPCR assays
    • Receptor Kinase assays
    • Ion channels
    • Transporter based assays
    • Proteasome inhibition assay (Ex-Vivo and Human PBMC)
    • Ex-vivo cell based and Gene expression studies
    • Platelet Aggregation Assay
    • BIAcore Binding Assays for Protein–Protein and Drug-Protein interactions

IN VIVO BIOLOGY

  • Evaluation of the biological effects and physiological effect of a drug in a complex living organism.
    To understand the drug candidate behaviour
    • Bioavailability
    • Pharmacokinetics,
    • Organ distribution,
    • Efficacy in animal models of disease, and
    • Potential toxicity of either the compound itself or its metabolite(s).
  • DiponeD CRS division has collaborated with reputed GLP accredited laboratory with animal facilities of several strains
    • Rat,
    • Mouse,
    • Guinei pig and Rabbit to execute in vivo pharmacology studies. Our scientific team has extensive experience helping patrons with the selection of appropriate animal models of disease, as well as collaborating to design new animal disease models to meet the specific needs of a drug discovery program.

IN VIVO BIOLOGY

  • We offer in vivo biology services in accordance with customer's-designed protocols supporting its discovery needs on flexible basis: from delivering standalone studies to taking over responsibility for planning and executing efficacy studies.
  • We offers early research and proof-of-principle pharmacology studies in relevant animal models of human diseases to assist your efficacy evaluations.
  • We can customize our in vivo pharmacology models to meet your unique objectives.

DRUG METABOLISM AND PHARMACOKINETICS (DMPK)

  • DiponEd provides comprehensive, cost-effective Drug Metabolism and Pharmacokinetics studies – DMPK Studies support across the drug discovery paradigm for evaluating and optimizing the drug-like properties of new chemical entities.
  • We provide DMPK services and bioanalytical/pharmacokinetic studies that span all stages of drug discovery,
  • Exploratory studies, Hit-to-lead, Lead optimization and Candidate selection, Preclinical IND-enabling studies. So, leverage on our ADME/DMPK services that help you make informed decisions.

DMPK

  • DMPK studies team basically comprises of
    • In Vitro,
    • In Vivo,
    • Met-ID and
    • Pre-formulation groups managed by highly experienced and matured scientific people.
  • We work closely with our clients to identify their requirements and clarify their expectations, including cost and time constraints.
  • We provid the following studies for DMPK solutions
    • In vitro drug metabolism of NCE (drug/new chemical entity):
  • Determination of metabolic stability, metabolic half life and Clearance prediction of NCE (new chemical entity or drug) in cross species (both rodent and non-rodent) liver/intestinal microsomes and hepatocytes.
  • Inhibition assays of NCE (drug/new chemical entity):
    • Determination of reversible IC50 in isoforms of CYPs and human liver microsomes:
    • C50 shift in liver microsomes:
    • Determination of Ki/Kinact in liver microsomes:
    • Determination of reversible IC50 in isoforms of UGTs and human liver microsomes
  • Plasma protein binding assay
  • Blood to plasma ratio determination
  • Whole blood and plasma stability
  • Pharmacokinetics studies in mice and rat are executed in our associated lab.

BIOTRANSFORMATION

  • Evaluation of the biological effects and physiological effect of a drug in a complex living organism.
    To understand the drug candidate behaviour
    • Bioavailability
    • Pharmacokinetics,
    • Organ distribution,
    • Efficacy in animal models of disease, and
    • Potential toxicity of either the compound itself or its metabolite(s).
  • Biotransformation support of NCE (drug/new chemical entity): Early drug discovery stage:
    Full biotransformation package of NCE to file ECN according to FDA guidelines
    • Full metabolite profile in cross species liver microsomes (both rodent and non-rodent: rat, mouse, dog, cyno and human).
    • Full metabolite profile in cross species hepatocytes (both rodent and non- rodent: rat, mouse, dog, cyno and human).
    • Metabolite identification in Aroclor induced rat liver S9.
    • Conducting bile duct cannulated rat study to understand metabolism and excretion pathways of NCE by using cold compound (which is not radio labeled): In that case full metabolite profile is determined in bile, urine, plasma and feces samples.
    • Detection of circulating metabolites in plasma samples (rat, mouse, dog and cyno).
    • Reaction phenotyping of NCE by using recombinant cytochrome P450s and specific chemical inhibitors. In some special cases reaction phenotying is also done by using recombinant UGTs.
    • Determination of non-cyp mediated metabolism like Aldehyde oxidase (AO) mediated metabolism of NCE by using human liver cytosol with/without AO inhibitor and Metabolomics

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