Description
Key facts
Detection method:Fluorescent,
Sample types:Tissue Lysate, Microsomes, Cell Lysate,
Assay type:Quantitative,
Assay Platform:Microplate reader
Product details:
CYP3A4 Activity Assay Kit (Fluorometric) (ab211076) allows rapid measurement of native or recombinant CYP3A4 activity in biological samples such as liver microsomes. The assay utilizes a non-fluorescent CYP3A4 substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 535/587 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. CYP3A4 specific activity is calculated by running parallel reactions in the presence and absence of the potent inhibitor Ketoconazole and subtracting any residual activity detected with the inhibitor present.
The kit contains enough reagents to perform 100 sets of paired reactions (in presence / absence of inhibitor).
This product is manufactured by BioVision, an Abcam company and was previously called K701 Cytochrome P450 3A4 (CYP3A4) Activity Assay Kit (Fluorometric). K701-200 is the same size as the 200 test size of ab211076.
Cytochrome P450 3A4 (CYP3A4, EC 1.14.13.157) is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolism enzymes. CYPs are membrane-bound hemeproteins responsible for Phase I biotransformation reactions, in which lipophilic drugs and other xenobiotic compounds are transformed to more hydrophilic products to facilitate excretion from the body. CYP3A4 is expressed in high levels in the liver and intestines, where it catalyzes oxidation of an extraordinarily wide variety of structurally distinct ligands. More than half of all small molecule drugs commonly used by humans are metabolized by CYP3A4. Inhibition of CYP3A4-mediated metabolism is a common cause of adverse drug/drug and drug/food interactions and toxicity. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form, CYP3A4 inhibition can lead to decreased drug efficacy.
The Safety Datasheet for this product has been updated for certain countries. Please check the current version in the Support and downloads section.
Properties and Storage Information:
Shipped at conditions-Blue Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information--20°C
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
CYP3A43 is an enzyme belonging to the cytochrome P450 superfamily also known by the alternate name Cytochrome P450 3A43. This enzyme has a molecular mass of approximately 57 kDa and features prominently in the metabolism of xenobiotics and drugs. CYP3A43 is mainly expressed in liver and small intestine tissues where it resides in the endoplasmic reticulum. It functions by oxidizing small foreign organic molecules such as toxins or drugs aiding in their clearance from the body.
Biological function summary
CYP3A43 plays significant roles in drug metabolism and synthesis of cholesterol steroids and other lipids. It does not appear to be part of a larger enzyme complex functioning independently within cells. Its activity is essential in transforming various substances into metabolites some of which are inactive while others may remain active. The enzyme is important for modulating the pharmacokinetics of drugs which includes absorption distribution metabolism and excretion of pharmaceutical compounds.
Pathways
CYP3A43 is involved in the xenobiotic metabolism pathway alongside other enzymes like CYP3A4 and CYP3A5. This pathway facilitates the detoxification of potentially harmful compounds. Additionally CYP3A43 participates in the metabolism of endogenous substrates contributing to the homeostasis of steroid hormones. Within these pathways it interacts with other cytochrome P450 enzymes sharing substantial substrate overlaps and sometimes competing with CYP3A4 which significantly influences the effects and side effects of drugs.
CYP3A43 has connections to alterations in drug metabolism that could lead to adverse drug reactions or ineffective therapy. Its variability in expression and activity can impact conditions such as cancer where drug metabolism is important for effective chemotherapy. Moreover the enzyme influences steroid hormone balance which may relate to disorders like hypertension or endocrine-related cancers. In these contexts CYP3A43 and related enzymes like CYP3A4 are pivotal in individual patient responses to drug treatments driving the need for personalized medicine approaches.
