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CYP1A2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

51

Inhibitors & Agonists

14

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4

Isotope-Labeled Compounds

1

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Art. -Nr. Produktname Target Forschungsgebiete Chemical Structure
  • HY-B0476
    Phenacetin
    1 Publications Verification

    Acetophenetidin

    		 COX Inflammation/Immunology
    Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin
  • HY-N0043
    Ginsenoside Rd
    1 Publications Verification

    Gypenoside VIII

    		 NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology Cancer
    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 Ca 2+ 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.
    Ginsenoside Rd
  • HY-111338
    Tacrine
    5+ Cited Publications

    		 Cholinesterase (ChE) Neurological Disease
    Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .
    Tacrine
  • HY-19340
    TMS
    Maximum Cited Publications
    9 Publications Verification

    (E)-2,3',4,5'-tetramethoxystilbene

    		 Cytochrome P450 Cancer
    TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
    TMS
  • HY-30152
    Xanthotoxol
    2 Publications Verification

    8-Hydroxypsoralen

    		 5-HT Receptor Reactive Oxygen Species (ROS) Endogenous Metabolite Neurological Disease Inflammation/Immunology
    Xanthotoxol (8-Hydroxypsoralen) It is a kind of fragrant bean substance, and it is a CYP450 inhibitor. Xanthotoxol has anti-inflammatory, anti-inflammatory, and 5-HT antagonistic and protective effects. Xanthotoxol inhibited CYP3A4 sum CYP1A2 IC50s separation 7.43 μM sum 27.82 μM. Xanthotoxol can pass through MAPK and NF-κB, inhibiting inflammation.
    Xanthotoxol
  • HY-17614
    Ezutromid

    SMT C1100; BMN 195; VOX-C1100

    		 Cytochrome P450 Others
    Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
    Ezutromid
  • HY-18063
    ML252

    		Potassium Channel Cytochrome P450 Neurological Disease
    ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant .
    ML252
  • HY-W013268
    (S)-(+)-N-3-Benzylnirvanol

    (+)-N-3-Benzylnirvanol

    		 Cytochrome P450 Metabolic Disease
    (S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 .
    (S)-(+)-N-3-Benzylnirvanol
  • HY-N1050
    Zederone

    		mTOR Ribosomal S6 Kinase (RSK) Bacterial Infection Neurological Disease Cancer
    Zederone is a sesquiterpene. Zederone inhibits ovarian cancer cell proliferation through mTOR/p70s6K signalling pathway. Zederone inhibits CYP activities with IC50s of 2.9 μM (CYP2B6), 9.2 μM (CYP2C9), 11,2 μM (CYP2C19) and >30 μM (CYP1A2 and CYP2D6). Zederone is hepatotoxic with LD50 value at 24 hours in mice of approximately 223 mg/kg and cytotoxic against the KG1a cell line. Zederone shows antibacterial activity against a number of multi-drug resistant and Methicillin (HY-121544)-resistant Staphylococcus aureus strain. Zederone shows cognition improving capacity and assists in the modulation of gut bacterial dysbiosis .
    Zederone
  • HY-W010195
    2,6-Dimethylquinoline

    		Cytochrome P450 Others
    2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM .
    2,6-Dimethylquinoline
  • HY-117026
    LKY-047
    1 Publications Verification

    		 Cytochrome P450 Metabolic Disease Inflammation/Immunology
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
    LKY-047
  • HY-132845
    Utreloxastat

    PTC857

    		 α-synuclein Cytochrome P450 Ferroptosis Lipoxygenase Neurological Disease
    Utreloxastat (PTC857) is an orally active and blood-brain barrier-permeable 15-lipooxygenase inhibitor. Utreloxastat is a weak inhibitor of CYP1A2 and 2B6 with an IC50 of >5.3 μM. Utreloxastat reduces oxidative stress and inhibits the consumption of reduced glutathione and ferroptosis. Utreloxastat can be used in the study of neurodegenerative diseases characterized by high levels of oxidative stress and mitochondrial pathology, such as amyotrophic lateral sclerosisc .
    Utreloxastat
  • HY-N2382
    Polyphyllin H
    1 Publications Verification

    		 Cytochrome P450 P-glycoprotein Metabolic Disease Cancer
    Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 μM, competitive), CYP2D6 (IC50 = 13.88 μM, competitive) and CYP3A4 (IC50 = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel .
    Polyphyllin H
  • HY-B0476S
    Phenacetin-d5

    Acetophenetidin-d5

    		 COX Inflammation/Immunology
    Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin-d5
  • HY-B0476R
    Phenacetin (Standard)
    1 Publications Verification

    Acetophenetidin (Standard)

    		 Reference Standards COX Inflammation/Immunology
    Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin (Standard)
  • HY-W045990
    2,7-Dimethylnaphthalene

    		Cytochrome P450 Metabolic Disease
    2,7-Dimethylnaphthalene is a selective cytochrome P450 1A2 (CYP1A2) enzyme inhibitor with an IC50 of 65 μM. 2,7-Dimethylnaphthalene can be used for the research of metabolic disease .
    2,7-Dimethylnaphthalene
  • HY-W777979
    Frutinone A

    		Cytochrome P450 Bacterial Infection
    Frutinone A is a CYP1A2 inhibitor, possesses a chromonocoumarin structural scaffold. Frutinone A shows various biological activities, including antibacterial and antioxidant .
    Frutinone A
  • HY-N8382
    Chalepensin

    		Cytochrome P450 Parasite Insecticide Infection
    Chalepensin is a nematicide and CYP inhibitor. Chalepensin inhibits CYP2A6, CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees, with IC50 values of 82.3 μM, 2.86 μM, 3.01 μM, 0.21 μM, 6.58 μM, 1.67 μM, 61.1 μM, and 61.7 μM, respectively. Chalepensin potently and selectively kills third-stage infective larvae of Strongyloides venezuelensis .
    Chalepensin
  • HY-W015697
    3-Methylquinoline

    		Cytochrome P450 Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    3-Methylquinoline is a selective cytochrome P450 (CYP1A2) inhibitor with an IC50 of 13 μM. 3-Methylquinoline can reduce the metabolic clearance of CYP1A2 substrate drugs. 3-Methylquinoline can inhibit the activation of carcinogenic precursors .
    3-Methylquinoline
  • HY-N3090
    Peucedanol

    		Cytochrome P450 Metabolic Disease
    Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
    Peucedanol
  • HY-N1882
    4,5-Dimethoxycanthin-6-one

    		Cytochrome P450 Metabolic Disease
    4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae) .
    4,5-Dimethoxycanthin-6-one
  • HY-B0476S1
    Phenacetin-13C

    		COX Inflammation/Immunology
    Phenacetin- 13C is the 13C labeled Phenacetin . Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin-13C
  • HY-131495
    (S)-6-O-Desmethylnaproxen

    (S)-6-Desmethyl Naproxen

    		 COX Inflammation/Immunology
    (S)-6-O-Desmethylnaproxen ((S)-6-Desmethyl Naproxen) is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (+)-naproxen ((S)-naproxen). (S)-6-O-Desmethylnaproxen is formed from (S)-naproxen by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2C9.
    (S)-6-O-Desmethylnaproxen
  • HY-155732
    NPD-2975

    		Parasite Infection
    NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
    NPD-2975
  • HY-175836
    CYP1B1-IN-12

    		Cytochrome P450 Apoptosis Cancer
    CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
    CYP1B1-IN-12
  • HY-124158
    KR-60436

    		Proton Pump Metabolic Disease
    KR-60436 is a reversible H +/K +-ATPase inhibitor. KR-60436 can potently inhibit the metabolism of CYP1A2 substrates .
    KR-60436
  • HY-W010195R
    2,6-Dimethylquinoline (Standard)

    		Reference Standards Cytochrome P450 Others
    2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM .
    2,6-Dimethylquinoline (Standard)
  • HY-156330
    HIV-IN-9

    		HIV Cytochrome P450 Infection
    HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .
    HIV-IN-9
  • HY-179154
    α-Glucosidase-IN-101

    		Glycosidase Cytochrome P450 Metabolic Disease
    α-Glucosidase-IN-101 (Compound 13j) is an uncompetitive α-glucosidase inhibitor, with an IC50 of 120 nM. α-Glucosidase-IN-101 properly inhibits CYP1A2, CYP2C19, and CYP2C9 isoforms of cytochrome P450. α-Glucosidase-IN-101 can be used in the research of diabetes .
    α-Glucosidase-IN-101
  • HY-111338R
    Tacrine (Standard)

    		Cholinesterase (ChE) Reference Standards Neurological Disease
    Tacrine (Standard) is the analytical standard of Tacrine. This product is intended for research and analytical applications. Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .
    Tacrine (Standard)
  • HY-143906
    URAT1 inhibitor 2

    		URAT1 Inflammation/Immunology
    URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout .
    URAT1 inhibitor 2
  • HY-123319A
    Antofloxacin

    		Bacterial Antibiotic Infection
    Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
    Antofloxacin
  • HY-123319
    Antofloxacin hydrochloride

    		Bacterial Antibiotic Infection
    Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
    Antofloxacin hydrochloride
  • HY-17614R
    Ezutromid (Standard)

    SMT C1100 (Standard); BMN 195 (Standard); VOX-C1100 (Standard)

    		 Cytochrome P450 Reference Standards Others
    Ezutromid (Standard) is the analytical standard of Ezutromid. This product is intended for research and analytical applications. Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
    Ezutromid (Standard)
  • HY-W707708
    N-(4-Ethoxyphenyl)acetamide-2,2,2-d3

    		Isotope-Labeled Compounds COX Inflammation/Immunology
    N-(4-Ethoxyphenyl)acetamide-2,2,2-d3 is the deuterium labeled Phenacetin (HY-B0476). Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    N-(4-Ethoxyphenyl)acetamide-2,2,2-d3
  • HY-106379
    Lurosetron

    GR-87442

    		 5-HT Receptor Neurological Disease
    Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM. .
    Lurosetron
  • HY-169119
    Antifungal agent 114

    		Cytochrome P450 Fungal 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 .
    Antifungal agent 114
  • HY-152079
    CYP1B1-IN-3

    		Cytochrome P450 Cancer
    CYP1B1-IN-3 is a potent and selective CYP1B1 inhibitor with IC50 values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways .
    CYP1B1-IN-3
  • HY-30152R
    Xanthotoxol (Standard)

    8-Hydroxypsoralen (Standard)

    		 Reference Standards 5-HT Receptor Reactive Oxygen Species (ROS) Endogenous Metabolite Neurological Disease Inflammation/Immunology
    Xanthotoxol (Standard) is the analytical standard of Xanthotoxol. This product is intended for research and analytical applications. Xanthotoxol (8-Hydroxypsoralen) It is a kind of fragrant bean substance, and it is a CYP450 inhibitor. Xanthotoxol has anti-inflammatory, anti-inflammatory, and 5-HT antagonistic and protective effects. Xanthotoxol inhibited CYP3A4 sum CYP1A2 IC50s separation 7.43 μM sum 27.82 μM. Xanthotoxol can pass through MAPK and NF-κB, inhibiting inflammation .
    Xanthotoxol (Standard)
  • HY-131495R
    (S)-6-O-Desmethylnaproxen (Standard)

    (S)-6-Desmethyl Naproxen (Standard)

    		 Cytochrome P450 Reference Standards Inflammation/Immunology
    (S)-6-O-Desmethylnaproxen (Standard) is the analytical standard of (S)-6-O-Desmethylnaproxen. This product is intended for research and analytical applications. (S)-6-O-Desmethylnaproxen ((S)-6-Desmethyl Naproxen) is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (+)-naproxen ((S)-naproxen). (S)-6-O-Desmethylnaproxen is formed from (S)-naproxen by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2C9.
    (S)-6-O-Desmethylnaproxen (Standard)
  • HY-173032
    VU6033685

    		mGluR Neurological Disease
    VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
    VU6033685
  • HY-172393
    TCF4/β-catenin-IN-1

    		β-catenin Apoptosis Caspase MDM-2/p53 Bcl-2 Family Cytochrome P450 Cancer
    TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells .
    TCF4/β-catenin-IN-1
  • HY-18063A
    ML252 hydrochloride

    		Potassium Channel Cytochrome P450 Neurological Disease
    ML252 hydrochloride is a selective inhibitor of KCNQ2 (Kv7.2) channel with IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 hydrochloride also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 hydrochloride shows highly brain penetrant .
    ML252 hydrochloride
  • HY-N0043R
    Ginsenoside Rd (Standard)

    Gypenoside VIII (Standard)

    		 Reference Standards NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology Cancer
    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.
    Ginsenoside Rd (Standard)
  • HY-174425
    CYP1B1-IN-9

    		Cytochrome P450 Cancer
    CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance .
    CYP1B1-IN-9
  • HY-178786
    RET-IN-31

    		RET Potassium Channel Cytochrome P450 Cancer
    RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RET WT, RET V804L, RET V804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers .
    RET-IN-31
  • HY-W142473
    1,2-Dimethylnaphthalene

    		Cytochrome P450 Others
    1,2-Dimethylnaphthalene is a CYP1A2 inhibitor with an IC50 of 5.5 μM and a pIC50 of 5.26 .
    1,2-Dimethylnaphthalene
  • HY-153875
    Saccharolactone

    		β-glucuronidase Cytochrome P450 Metabolic Disease
    Saccharolactone is a potent orally active β-glucuronidase inhibitor. Saccharolactone markedly lowers biliary endogenous β-glucuronidase activity in the rat bile. Saccharolactone can stabilize glucuronide metabolites in vitro. Saccharolactone is also a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms (IC50 < 4 mM) .
    Saccharolactone
  • HY-B0476S3
    Phenacetin-13C-1

    Acetophenetidin-13C-1

    		 Isotope-Labeled Compounds COX Endogenous Metabolite Ferroptosis Inflammation/Immunology
    Phenacetin- 13C-1 (Acetophenetidin- 13C-1) is the 13C-labeled Phenacetin (HY-B0476). Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin-13C-1
  • HY-181747
    CYP11A1-IN-3

    		Cytochrome P450 Cancer
    CYP11A1-IN-3 (Compound II-4) is a selective CYP11A1 inhibitor with an IC50 of 26.7 nM. CYP11A1-IN-3 shows selectivity towards CYP1A2, 2C9 and 2D6. CYP11A1-IN-3 can be used for the research of castration-resistant prostate cancer .
    CYP11A1-IN-3

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