101 Results for "

Human CYP3A4

" in MedChemExpress (MCE) Product Catalog:
Products (101)

101 Results for "Human CYP3A4" in MCE Product Catalog:

36
36 Publications Verification
Cat. No.: HY-17356
CAS No.: 49562-28-9
Domaines de recherche:  

Cardiovascular Disease Cancer

Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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14
14 Cited Publications
Cat. No.: HY-N6972
CAS No.: 481-49-2
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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4
4 Cited Publications
Cat. No.: HY-N2259
CAS No.: 19431-84-6
Synonyms: (+)-Curcumenol
Curcumenol ((+)-Curcumenol) is a natural compound with oral efficacy, exhibiting an IC50 of 12.6 μM and a Ki of 10.8 μM against human CYP3A4. Curcumenol inhibits TNFα-induced phosphorylation/degradation of IκBα, phosphorylation/nuclear translocation of NF-κB p65, as well as the upregulation of MMP3, MMP9, MMP13, TRAF3, IL1RL1, TNFα and IL-1β. Curcumenol suppresses LPS-induced phosphorylation of Akt and p38 MAPK, as well as the production of pro-inflammatory mediators/proteins, and downregulates the SLC7A11/NF-κB/TGF-β pathway. Curcumenol binds to and inhibits the activation of Fyn and Lyn, blocks the function of downstream FcεRI signaling components, and reduces the release of allergic mediators/cytokines. Curcumenol upregulates the expression of KDM6B, and promotes chondrocyte proliferation and cartilage repair. Curcumenol induces ferroptosis and apoptosis, regulates the EMT process, and inhibits tumor growth and metastasis of triple-negative breast cancer. Curcumenol possesses anti-inflammatory, neuroprotective, antioxidant, antitumor, antiviral and hepatoprotective activities. Curcumenol can be used in research related to intervertebral disc degeneration, cancer, inflammation, central nervous system neurodegenerative diseases, allergic reactions and knee osteoarthritis .
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3
3 Cited Publications
Cat. No.: HY-100386
CAS No.: 55142-85-3
Pureté:  99.56%
Synonyms: PCR 5332
Target:  

NTPDase Cytochrome P450

Domaines de recherche:  

Cardiovascular Disease

Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
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3
3 Cited Publications
Cat. No.: HY-B0153A
CAS No.: 53885-35-1
Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
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3
3 Cited Publications
Cat. No.: HY-N6065
CAS No.: 73069-27-9
Synonyms: (+)-Praeruptorin A
Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension .
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2
2 Cited Publications
Cat. No.: HY-G0006
CAS No.: 73590-85-9
Synonyms: Ufiprazole
Omeprazole sulfide (Ufiprazole) is a metabolic degradation product of Omeprazole (HY-B0113). Omeprazole sulfide acts as a modulator of AhR. Omeprazole sulfide in cells with low CYP3A4 expression, functions as an AhR antagonist; however, in cells with high CYP3A4 expression, it is rapidly metabolized to Omeprazole, thereby acting as an AhR agonist. Omeprazole sulfide exhibits antibacterial activity when conjugated with silver nanoparticles (AgNPs). Omeprazole sulfide can be used in research on acid suppression and bacterial infections .
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2
2 Cited Publications
Cat. No.: HY-10505
CAS No.: 566939-85-3
Pureté:  99.70%
Synonyms: TAK-700
Target:  

Cytochrome P450

Domaines de recherche:  

Cancer

Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4 .
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1
1 Cited Publications
Cat. No.: HY-N2411
CAS No.: 60314-89-8
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT1A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ 3H]8-OH-DPAT to the 5-HT1A receptor in a concentration-dependent manner, with an IC50 of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .
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1
1 Cited Publications
Cat. No.: HY-126562
CAS No.: 5950-12-9
Pureté:  99.31%
Piperlonguminine is a cytochrome P450 (CYP450) inhibitor. Piperlonguminine also inhibits the growth of epimastigotes and intracellular amastigotes of Trypanosoma cruzi, with IC50 values of 53.8 and 33.9 μM, respectively . Piperlonguminine regulates HMGB1/TLR4-NF-κB/MAPK-related inflammatory responses, endothelial protein C receptor (EPCR) shedding, melanogenesis, glycolipid metabolism, ischemic brain injury and tumor growth. Piperlonguminine can be used in research on hyperlipidemia, sepsis, Chagas disease, ischemic stroke, sarcoma and severe acute pancreatitis-associated lung injury .
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1
1 Cited Publications
Cat. No.: HY-112690A
CAS No.: 625095-61-6
Pureté:  99.53%
Synonyms: Remofovir mesylate
Target:  

Cytochrome P450

Domaines de recherche:  

Infection Metabolic Disease

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
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1
1 Cited Publications
Cat. No.: HY-P74210
Pureté:  ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CYP3A4; CYPIIIA3; Prev. CYP3A3; Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 3; Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 4; Taurochenodeoxycholate 6-Alpha-Hydroxylase; Cytochrome P450, Family 3, Subfamily A,
Species:  
Human
Source:  
E. coli
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Cat. No.: HY-109171
CAS No.: 929046-33-3
Pureté:  99.82%
Synonyms: NT-814; BAY3427080
Target:  

Neurokinin Receptor

Domaines de recherche:  

Cardiovascular Disease Neurological Disease

Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
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Cat. No.: HY-B0822
CAS No.: 120068-37-3
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .
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Cat. No.: HY-157421
CAS No.: 2847156-05-0
Target:  

NAMPT

Domaines de recherche:  

Metabolic Disease

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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Cat. No.: HY-16265
CAS No.: 900573-88-8
Domaines de recherche:  

Cancer

JI-101 is an orally active multi-kinase inhibitor. JI-101 inhibits EphB4, VEGFR-2 and PDGFR-β. JI-101 exhibits anticancer activity. JI-101 can be used in research related to ovarian cancer .
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Cat. No.: HY-N5132
CAS No.: 7787-20-4
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .
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Cat. No.: HY-19958
CAS No.: 912656-34-9
Target:  

Sodium Channel

Domaines de recherche:  

Neurological Disease

XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain .
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Cat. No.: HY-113482
CAS No.: 80434-32-8
Synonyms: 1β-OH-DCA
1β-Hydroxydeoxycholic acid (1β-OH-DCA), a secondary bile acid, is a CYP3A biomarker. Deoxycholic acid is specifically metabolized into 1β-Hydroxydeoxycholic acid by CYP3A4 and CYP3A7 using recombinant human CYP450 enzymes .
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Cat. No.: HY-128914
CAS No.: 1943604-24-7
Pureté:  99.53%
Domaines de recherche:  

Cancer

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 .
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