CYP3A4 Activity Assay Kit (Fluorometric) (ab211076) allows rapid measurement of native or recombinant CYP3A4 activity in biological samples such as liver microsomes.
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- RSC advances 12:19431-194442022Coupling of acceptor-substituted diazo compounds and tertiary thioamides: synthesis of enamino carbonyl compounds and their pharmacological evaluation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJim Secka,Arpan Pal,Francis A Acquah,Blaine H M Mooers,Anand B Karki,Dania Mahjoub,Mohamed K Fakhr,David R Wallace,Takuya Okada,Naoki Toyooka,Adama Kuta,Naga Koduri,Deacon Herndon,Kenneth P Roberts,Zhiguo Wang,Bethany Hileman,Nisha Rajagopal,Syed R HussainiPubMed 35865562
- Frontiers in bioengineering and biotechnology 10:8260932022Application of 3D Hepatic Plate-Like Liver Model for Statin-Induced Hepatotoxicity Evaluation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJiecheng Xu,Daogang Pan,Wei Liao,Zhidong Jia,Mingxin Pan,Jun Weng,Xu Han,Shao Li,Yang Li,Kangyan Liang,Shuqin Zhou,Qing Peng,Yi GaoPubMed 35372314
- Journal of medicinal chemistry 64:8437-84462021Carbon Monoxide Inhibits Cytochrome P450 Enzymes CYP3A4/2C8 in Human Breast Cancer Cells, Increasing Sensitivity to Paclitaxel.Applications:Unspecified applicationReactive species:Unspecified reactive speciesBrian Kawahara,Kym F Faull,Carla Janzen,Pradip K MascharakPubMed 34097831
Key facts
- Detection method
Fluorescent
- Sample types
Tissue Lysate, Microsomes, Cell Lysate
- Assay type
Quantitative
- Reactive species
Mammals
Target data
Function
Exhibits low testosterone 6-beta-hydroxylase activity.
Alternative names
Cytochrome P450 3A43, CYP3A43
What's included?
Recommended products
CYP3A4 Activity Assay Kit (Fluorometric) (ab211076) allows rapid measurement of native or recombinant CYP3A4 activity in biological samples such as liver microsomes.
Alternative names
Cytochrome P450 3A43, CYP3A43
Key facts
- Detection method
Fluorescent
- Sample types
Tissue Lysate, Microsomes, Cell Lysate
- Assay type
Quantitative
- Reactive species
Mammals
- Assay Platform
Microplate reader
Storage
- Shipped at conditions
Blue Ice
- Appropriate short-term storage conditions
-20°C
- Appropriate long-term storage conditions
-20°C
- Storage information
-20°C
Notes
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.
Supplementary info
This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
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.
- Associated diseases and disorders
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.
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3 product images
Functional Studies - CYP3A4 Activity Assay Kit (Fluorometric) (ab211076)
Typical Resorufin standard calibration curve. One mole of resorufin corresponds to the metabolism of one mole of CYP3A4 substrate.
Functional Studies - CYP3A4 Activity Assay Kit (Fluorometric) (ab211076)
Reaction kinetics of fluorogenic substrate metabolism in human liver microsomes (0.05 mg/mL) at 37°C in the presence and absence of the CYP3A4 inhibitor Ketoconazole ("no inhibitor" reaction contained a final concentration of 0.6% acetonitrile).
Functional Studies - CYP3A4 Activity Assay Kit (Fluorometric) (ab211076)
Specific activity of CYP3A4 in pooled human liver microsomes (0.05 mg/mL).
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