In Vitro Phenotyping Assay Service

The phenotyping assays are a key component of in vitro ADME screening services to assess the metabolic pathway(s) responsible for the biotransformation of a particular drug candidate or compound. These assays help determine the enzymes, such as cytochrome P450s (CYPs) or UDP-glucuronosyltransferases (UGTs), involved in the metabolism of a compound, as well as predict potential drug-drug interactions or metabolic liabilities.

At Creative Biolabs, we offer in vitro reaction phenotyping assays including:

CYP Phenotyping Assay

At Creative Biolabs, we provide in vitro CYP phenotyping assay services to assess if a test compound is a substrate for the specific CYP enzyme. Our expert team utilizes well-established techniques to measure the intrinsic clearance of compounds by specific CYP enzymes, providing valuable information on the potential metabolic fate of tested compounds.

  • In vitro CYP2C9 intrinsic clearance measurement
  • In vitro CYP2C19 intrinsic clearance measurement
  • In vitro CYP2D6 intrinsic clearance measurement
  • In vitro CYP3A4 intrinsic clearance measurement
  • In vitro CYP2C8 intrinsic clearance measurement
  • In vitro CYP2B6 intrinsic clearance measurement
  • In vitro CYP1A2 intrinsic clearance measurement

UGT Phenotyping Assay

Our in vitro UGT phenotyping assay service involves the assessment of the enzymatic activity of UGTs using appropriate substrates. This assay helps in determining the clearance rates of UGT enzymes, which play a crucial role in the metabolism of drugs and other xenobiotics.

  • In vitro UGT1A1 intrinsic clearance measurement
  • In vitro UGT1A3 intrinsic clearance measurement
  • In vitro UGT1A4 intrinsic clearance measurement
  • In vitro UGT1A6 intrinsic clearance measurement
  • In vitro UGT1A8 intrinsic clearance measurement
  • In vitro UGT1A9 intrinsic clearance measurement
  • In vitro UGT1A10 intrinsic clearance measurement
  • In vitro UGT2B4 intrinsic clearance measurement
  • In vitro UGT2B7 intrinsic clearance measurement
  • In vitro UGT2B15 intrinsic clearance measurement

Transporter Substrate Assessment

Transporter substrate assessment service involves assessing the compound's interaction with various transporters such as P-glycoprotein (P-gp), multidrug resistance protein (MRP), and breast cancer resistance protein (BCRP), among others. This assay evaluates the ability of the test compound to cross a cellular barrier in a directional manner (apical to basolateral and basolateral to apical) and provides insights into whether the compound is a substrate of the specific transporter.

  • MATE substrate assessment
  • Caco-2-based MRP2 substrate assessment
  • Caco-2-based P-gp substrate assessment
  • MDCKII-based P-gp substrate assessment
  • CHO-K1-based OATP1B1 substrate assessment
  • CHO-K1-OATP1B3 substrate assessment
  • Cell-based ASBT substrate assessment
  • Caco-2-based BCRP substrate assessment
  • Caco-2-based Efflux Transporter substrate assessment

Cell-based Cytotoxicity Safety Screening

We also provide a large menu of cell-based cytotoxicity safety assessments to evaluate the potential toxicity of compounds. This includes assessing the impact of compounds on cell viability and proliferation, which can be crucial information for drug safety evaluations.

  • BJ cell-based cytotoxicity safety screening
  • HEK293-based cytotoxicity safety screening
  • H4-l-E-C3-based cytotoxicity safety screening
  • HepG2-based cytotoxicity safety screening
  • HUVEC-based cytotoxicity safety screening
  • Jurkat cell-based cytotoxicity safety screening
  • MRC-5-based cytotoxicity safety screening

Cell-based Drug-Induced Liver Injury Screening

At Creative Biolabs, we provide cell-based drug-induced liver injury assays specifically designed to rapidly screen compounds for potential liver toxicity using human primary cells. Our liver injury assays, which primarily measure cell viability, offer valuable insights into the potential hepatotoxicity of pharmaceutical compounds, enabling early identification and mitigation of harmful effects on the liver.

Nuclear Receptor Assay

We offer various cell-based nuclear receptor assays to examine the effects of drugs on nuclear receptor activity. Our assays cover a wide range of nuclear receptors such as aryl hydrocarbon receptors (AhR), pregnane X receptors (PXR), constitutive androstane receptor-3 (CAR3), and others. These assays provide valuable insights into the interactions between drugs and nuclear receptors, aiding in drug development and toxicity screening.

As an expert in drug development, Creative Biolabs delivers both in vitro ADME and in vivo DMPK services for cancer immunotherapy, including high-throughput ADME, metabolic stability, plasma protein binding, in vivo PK, and more. Contact us to discuss your ADME project.

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