Search Result
Results for "
CYP3A4 activity
" in MedChemExpress (MCE) Product Catalog:
7
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N0598
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20(S)-Ginsenoside F1
|
Cytochrome P450
Endogenous Metabolite
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Cancer
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Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
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-
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- HY-135331
-
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Androgen Receptor
Cytochrome P450
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Cancer
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N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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-
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- HY-119804
-
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Cytochrome P450
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Neurological Disease
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Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
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-
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- HY-18642
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PF-4981517
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Cytochrome P450
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Others
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CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism .
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- HY-168210
-
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Fungal
Cytochrome P450
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Infection
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Antifungal agent 122 (compound 201) is a potent and broad-spectrum antifungal agent. Antifungal agent 122 prevents fungal phase transition and the formation of fungal biofilm. Antifungal agent 122 inhibits CYP3A4-M and CYP3A4-T enzyme activity with IC50 values of 2.11, 4.53 µM. Antifungal agent 122 shows no cytotoxicity .
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-
-
- HY-121057
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3-OH FNTZ
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Drug Metabolite
Cytochrome P450
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Metabolic Disease
|
3-Hydroxyflunitrazepam (3-OH FNTZ) is the major metabolite of Flunitrazepam (FNTZ), generated via 3-hydroxylation by CYP3A4 (Km = 286 μM), and represents the dominant metabolic pathway (>80%) in liver microsomes. Its formation is significantly inhibited by CYP3A4 inhibitors such as Ketoconazole (HY-B0105) (IC50 = 0.11 μM) and Ritonavir (HY-90001) (IC50 = 0.041 μM), indicating a strong dependence on CYP3A4 activity and potential drug interactions .
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-
-
- HY-163324A
-
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Cytochrome P450
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Others
|
2-Me PeER is a rhodamine dye-based fluorescent probe that detects CYP3A4 activity. In fluorescence-activated cell sorting (FACS) based on CYP3A4 activity, homogeneous and functional human induced pluripotent stem cell (hiPSC)-derived hepatocytes and intestinal epithelial cells can be obtained with the aid of 2-Me PeER .
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-
-
- HY-121580
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NN703
|
Cytochrome P450
|
Endocrinology
|
Tabimorelin (NN703) is an orally active growth hormone (GH) secretagogue. Tabimorelin is also a potent inhibitor of CYP3A4 activity .
|
-
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- HY-163324
-
|
Fluorescent Dye
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Others
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2-Me PeER (chloride) is a fluorogenic probe for CYP3A4 activity that can be used in living cells . Ex / Em = 520 / 550 nm
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-
-
- HY-103540
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NN703 hemifumarate
|
Cytochrome P450
|
Endocrinology
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Tabimorelin (NN703) hemifumarate is an orally active growth hormone (GH) secretagogue. Tabimorelin hemifumarate is also a potent inhibitor of CYP3A4 activity .
|
-
-
- HY-N0893S
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-
-
- HY-120425
-
|
Insecticide
|
Infection
|
Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mouse brain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
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-
-
- HY-N9434
-
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Cytochrome P450
|
Metabolic Disease
|
5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that inhibits hepatic testosterone 6β-hydroxylation (CYP3A4) activity with an IC50 of 7.8 μM .
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-
-
- HY-14874
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FYX-051
|
Xanthine Oxidase
Cytochrome P450
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Metabolic Disease
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Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
|
-
-
- HY-N0144
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-
-
- HY-14273
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BAL-4815; RO-0094815
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Fungal
Cytochrome P450
Antibiotic
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Infection
Cancer
|
Isavuconazole (BAL-4815) is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
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-
-
- HY-12433
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-
-
- HY-W754151
-
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Isotope-Labeled Compounds
|
Others
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N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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-
-
- HY-100665
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OPC-14857; DM-14857
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5-HT Receptor
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Neurological Disease
|
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
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-
-
- HY-113575
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OPC-14857 hydrochloride; DM-14857 hydrochloride
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5-HT Receptor
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Neurological Disease
|
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .
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- HY-149977
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Cytochrome P450
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Cancer
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Anticancer agent 111 (compound 11) is a potent cytochrome P450 inhibitor with an IC50 value of 3 μM for CYP3A4. Anticancer agent 111 has anticancer activity. Anticancer agent 111 can be used in research of cancer .
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- HY-120425R
-
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Insecticide
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Infection
|
Ethiprole (Standard) is the analytical standard of Ethiprole. This product is intended for research and analytical applications. Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mouse brain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
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-
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- HY-135331S
-
|
Isotope-Labeled Compounds
Androgen Receptor
Cytochrome P450
|
Cancer
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N-Desmethyl-Apalutamide-15N,d4 is the 15N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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-
-
- HY-17508
-
|
Bacterial
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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-
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- HY-14874S
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FYX-051-d4
|
Isotope-Labeled Compounds
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
|
-
-
- HY-14751
-
SCH619734
|
Neurokinin Receptor
|
Neurological Disease
Cancer
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Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
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- HY-14751A
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SCH619734 hydrochloride
|
Neurokinin Receptor
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Neurological Disease
Cancer
|
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model .
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-
-
- HY-16436
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SCH619734 hydrochloride hydrate
|
Neurokinin Receptor
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Neurological Disease
Cancer
|
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .
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-
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- HY-14874R
-
|
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
Topiroxostat (Standard) is the analytical standard of Topiroxostat. This product is intended for research and analytical applications. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
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-
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- HY-N0598R
-
|
Cytochrome P450
Endogenous Metabolite
|
Cancer
|
Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
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-
-
- HY-12035
-
AMG-208
1 Publications Verification
|
c-Met/HGFR
Cytochrome P450
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Cancer
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AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity .
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-
- HY-130606
-
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NAMPT
Cytochrome P450
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Cancer
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Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively .
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- HY-W654320
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-
-
- HY-100665S
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OPC-14857-d8; DM-14857-d8
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Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
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Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
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- HY-N0144R
-
|
P-glycoprotein
Autophagy
Endogenous Metabolite
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Inflammation/Immunology
Cancer
|
Piperine (Standard) is the analytical standard of Piperine. This product is intended for research and analytical applications. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL .
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- HY-149813
-
|
P-glycoprotein
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Cancer
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P-gp inhibitor 14 (Compound 8a) is a high affinity P-gp inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC50=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity .
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-
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- HY-14273R
-
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Fungal
Cytochrome P450
Antibiotic
|
Infection
|
Isavuconazole (Standard) is the analytical standard of Isavuconazole. This product is intended for research and analytical applications. Isavuconazole (BAL-4815) is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
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-
-
- HY-D0146
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BzRes; 7-Benzyloxyresorufin; 7-Benzyloxyphenoxazone
|
Fluorescent Dye
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Others
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Resorufin benzyl ether (BzRes), a fluorogenic enzyme substrate, can be used to detect CYP3A4 enzyme activity. Resorufin benzyl ether modified with a recognizing moiety boronate, can be used for ONOO - detection via a self-immolation mechanism. Ex/Em=530-570 nm/590 nm .
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-
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- HY-100665R
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OPC-14857 (Standard); DM-14857 (Standard)
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5-HT Receptor
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Neurological Disease
|
Dehydroaripiprazole (Standard) is the analytical standard of Dehydroaripiprazole. This product is intended for research and analytical applications. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
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-
-
- HY-14294
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S-1153
|
Reverse Transcriptase
HIV
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Infection
|
Capravirine (S-1153) is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent antiviral activity. Capravirine inhibits replication of HIV-1 strains that are resistant to nucleoside/nucleotide reverse transcriptase inhibitors and other NNRTIs. Capravirine is metabolized by the cytochrome P450 enzyme CYP3A4 .
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- HY-17508S1
-
|
Isotope-Labeled Compounds
Bacterial
Antibiotic
Autophagy
Cytochrome P450
|
Others
|
Clarithromycin-d3 is the deuterium labeled Clarithromycin (HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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-
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- HY-17508R
-
|
Bacterial
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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-
-
- HY-W157689
-
|
Proteolytic Enzyme
|
Infection
Metabolic Disease
Cancer
|
IDE-IN-3 (Compound 4) is an inhibitor for insulin-degrading enzyme. IDE-IN-3 is predicted to have CYP3A4, CYP2C19, hERG, NADP+, HIF1α and histidine kinase inhibitory activities, and has potential biological activity in anti-diabetic, anti-tumor, anti-bacterial aspects, according to the in silico prediction .
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-
-
- HY-153989
-
|
Ras
Cytochrome P450
|
Cancer
|
SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitory activity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research .
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-
-
- HY-14751R
-
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
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-
-
- HY-117010
-
|
Cytochrome P450
HSV
SGLT
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Infection
Metabolic Disease
|
Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM . Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM) . Kushenol K also inhibits the activity of SGLT1 and SGLT2 .
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-
-
- HY-N2259
-
(+)-Curcumenol
|
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
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-
-
- HY-146458
-
|
Bacterial
Cytochrome P450
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Infection
|
Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice .
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-
-
- HY-W011235
-
|
5-HT Receptor
Calcium Channel
Drug Metabolite
|
Cardiovascular Disease
Neurological Disease
|
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity .
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-
- HY-147999
-
|
Bacterial
Fungal
Cytochrome P450
|
Infection
|
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
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- HY-169119
-
|
Cytochrome P450
Fungal
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Infection
|
Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .
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- HY-132866
-
|
P-glycoprotein
|
Cancer
|
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
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- HY-116862
-
DBF
|
Cytochrome P450
Fluorescent Dye
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Others
|
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
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- HY-112142A
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DVR-23
|
HBV
|
Inflammation/Immunology
|
(Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .
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- HY-13404
-
Capmatinib
Maximum Cited Publications
14 Publications Verification
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-13404B
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INC280 hydrochloride; INCB-28060 hydrochloride
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c-Met/HGFR
Apoptosis
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Cancer
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
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-
- HY-13404C
-
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
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Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
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-
- HY-13404A
-
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-W587878
-
|
Cytochrome P450
Pyruvate Kinase
Fungal
Apoptosis
Insecticide
|
Infection
Cancer
|
Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation .
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- HY-12946A
-
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
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- HY-12946
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Glucocorticoid Receptor
Cytochrome P450
HCV Protease
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Infection
Inflammation/Immunology
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BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
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- HY-N0043
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- HY-13404R
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c-Met/HGFR
Apoptosis
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Cancer
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Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
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- HY-N0043R
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Gypenoside VIII (Standard)
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NF-κB
COX
Calcium Channel
Cytochrome P450
Endogenous Metabolite
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
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- HY-N6972
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Infection
Inflammation/Immunology
Cancer
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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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- HY-N6972R
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Infection
Inflammation/Immunology
Cancer
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Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. 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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- HY-142942
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Glucocorticoid Receptor
MMP
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Inflammation/Immunology
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Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV .
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- HY-142941
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Glucocorticoid Receptor
MMP
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Inflammation/Immunology
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Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV .
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- HY-149247
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability .
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- HY-168528
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P-glycoprotein
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Cancer
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WS-917 is a potent and orally active ABCB1 modulator. WS-917 enhances ABCB1 ATPase activity. WS-917 significantly enhances the antitumor effect of paclitaxel combined with anti-PD-1 antibody. WS-917 promotes CD8 + T-cell activation .
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Cat. No. |
Product Name |
Type |
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- HY-116862
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DBF
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Fluorescent Dyes/Probes
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Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
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- HY-D0146
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BzRes; 7-Benzyloxyresorufin; 7-Benzyloxyphenoxazone
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Dyes
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Resorufin benzyl ether (BzRes), a fluorogenic enzyme substrate, can be used to detect CYP3A4 enzyme activity. Resorufin benzyl ether modified with a recognizing moiety boronate, can be used for ONOO - detection via a self-immolation mechanism. Ex/Em=530-570 nm/590 nm .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-W754151
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N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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- HY-N0893S
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Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
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- HY-135331S
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N-Desmethyl-Apalutamide-15N,d4 is the 15N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
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- HY-14874S
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Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
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- HY-W654320
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Piperin-d10 is deuterium labeled Piperine. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL .
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- HY-100665S
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Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
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- HY-17508S1
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Clarithromycin-d3 is the deuterium labeled Clarithromycin (HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
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