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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
41 Results for "
human CYP2D6
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "human CYP2D6" in MCE Product Catalog:
3
3 Cited Publications
Cat. No.: HY-18719
CAS No.: 112093-28-4
Research Areas:
Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
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3 Cited Publications
Cat. No.: HY-18719A
CAS No.: 1032008-74-4
Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
2
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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Cardiovascular Disease Alkaloids other families Metabolic Disease Nelumbo nucifera Gaertn. Plants Disease Research Fields Isoquinoline Alkaloids Nymphaeaceae
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Cat. No.: HY-157421
CAS No.: 2847156-05-0
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Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
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Other Monoterpenes Terpenoids Other Diseases Plants Umbelliferae Vernonia Schreb. Disease Research Fields
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Cat. No.: HY-W040468
CAS No.: 92321-29-4
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2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM) .
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Tubulysin is a microtubule destabilizer that binds to the β-tubulin peptide site adjacent to the vinca alkaloid binding site and inhibits tubulin polymerization. Tubulysin induces apoptosis and exhibits antiproliferative activity against a variety of human cancer cells, including multidrug-resistant strains. Tubulysin can be conjugated to antibodies via a disulfide-containing quaternary ammonium linker for ADC synthesis . Tubulysin is applicable to tumor-related research .
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
Cat. No.: HY-16718
CAS No.: 1044535-52-5
Synonyms: PF-00251802
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Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
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4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Cat. No.: HY-RS03461
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CYP2D6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2D6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Cardiovascular Disease Alkaloids Other Alkaloids Ranunculaceae Aconitum carmichaeli Debx. Plants Disease Research Fields
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Synonyms: BAY 1902607
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Filapixant (BAY 1902607) is an orally active and selective P2X3 receptor antagonist. Filapixant is applicable to the research of refractory chronic cough .
Cat. No.: HY-18719S
CAS No.: 1584173-54-5
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MK-3697 is an orally active orexin 2 receptor (OX2R) antagonist, with an IC50 value of 16 nM and a Ki value of 1.1 nM against human OX2R. MK-3697 blocks the wake-promoting OX2R signaling pathway, reduces active wake time, and increases slow-wave sleep and rapid eye movement sleep time in mice, rats and dogs. MK-3697 can be used for research on insomnia .
Cat. No.: HY-E72100
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Human CYP2D6, Reductase+b5 refers to a near-physiological recombinant microsomal system co-expressed in insect cells, consisting of human cytochrome P450 2D6, NADPH-P450 oxidoreductase (CPR) and cytochrome b5. Human CYP2D6 is a human cytochrome P450 subtype belonging to the CYP2 family, and also serves as a major metabolic enzyme capable of crossing the blood-brain barrier. Its expression is centered in the human liver (also detected in the brain) and exhibits high polymorphism .
Cat. No.: HY-169728
CAS No.: 378197-09-2
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SID 24785302 is a hexokinase inhibitor with antiparasitic activity. SID 24785302 exhibits activity against T. brucei and Leishmania. SID 24785302 can be used for the research of mitochondrial DNA disorders and parasitic infection .
Cat. No.: HY-16718A
CAS No.: 1044535-61-6
Synonyms: PF-00251802 hydrochloride
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Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
Cat. No.: HY-100064R
CAS No.: 847949-49-9
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O-Desmethyl gefitinib (Standard) is the analytical standard of O-Desmethyl gefitinib. This product is intended for research and analytical applications. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
