Search Result
Results for "
liver cytochrome
" in MedChemExpress (MCE) Product Catalog:
20
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-N6972
-
Cepharanthine
Maximum Cited Publications
13 Publications Verification
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
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 .
|
-
-
- HY-B0476
-
|
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 .
|
-
-
- HY-100386
-
|
PCR 5332
|
NTPDase
Cytochrome P450
|
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.
|
-
-
- HY-125348
-
|
|
Drug Metabolite
|
Cancer
|
|
6α-Hydroxy paclitaxel is one of the main metabolites of Paclitaxel (PTX) (HY-B0015), and it is generated by the liver cytochrome P450 enzyme CYP2C8. 6α-Hydroxy paclitaxel has bone marrow toxicity, but it can enhance the cytotoxicity of PTX against leukemia cells without causing cell toxicity. 6α-Hydroxy paclitaxel can be used in leukemia research .
|
-
-
- HY-B0153A
-
|
|
NTPDase
Cytochrome P450
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
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 .
|
-
-
- HY-129105
-
|
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
|
Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
|
-
-
- HY-157421
-
|
|
NAMPT
|
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 .
|
-
-
- HY-B1311
-
|
SKF-525A; U-5446; RP-5171
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
|
-
-
- HY-N2181
-
|
|
Cytochrome P450
Apoptosis
Bacterial
Autophagy
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD) .
|
-
-
- HY-N1431
-
|
|
NOD-like Receptor (NLR)
Apoptosis
Cytochrome P450
NF-κB
PI3K
Akt
CDK
Caspase
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer .
|
-
-
- HY-13568
-
|
LRCL 3794
|
Cytochrome P450
COX
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms .
|
-
-
- HY-N5132
-
|
|
Cytochrome P450
|
Others
|
|
(-)-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 .
|
-
-
- HY-A0069
-
|
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-B0885
-
|
(±)-Econazol
|
Fungal
Bacterial
Calcium Channel
Cytochrome P450
|
Infection
Metabolic Disease
|
|
Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
|
-
-
- HY-122652
-
|
|
Apoptosis
Aldose Reductase
|
Neurological Disease
Cancer
|
|
MitoBloCK-6 is a potent Erv1/ALR inhibitor, with an IC50 of 900 nM and 700 nM, respectively. MitoBloCK-6 also inhibits Erv2 (IC50=1.4 μM). MitoBloCK-6 can induce Apoptosis via cytochrome c release. MitoBloCK-6 inhibits growth of developing zebrafish motor neurons. MitoBloCK-6 has anticancer activity against liver cancer and leukemia .
|
-
-
- HY-Y0496
-
|
|
Insecticide
Environmental Pollutants
Mitosis
|
Cancer
|
1,4-Dichlorobenzene is a non-genotoxic, orally active mitogenic/tumor-promoting carcinogen that is also widely used as a dye, resin intermediate, and deodorant, moth repellent/insecticide. 1,4-Dichlorobenzene induces liver tumors in mice and promotes the growth of spontaneous precancerous lesions, but shows no liver tumor-inducing activity in F344 rats. Exposure to 1,4-dichlorobenzene leads to elevated leukocyte counts, serum alanine aminotransferase, and blood urea nitrogen levels. Due to the hepatotoxic characteristics, 1,4-Dichlorobenzene is applicable to liver cancer-related research .
|
-
-
- HY-125904
-
|
|
RAR/RXR
UGT
Cytochrome P450
Apoptosis
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
4-Hydroxyretinoic acid (4-HRA) is a derivative of Retinoic acid (HY-14649). 4-Hydroxyretinoic acid is formed via the catalysis of retinol by cytochrome P-450 isoenzymes. 4-Hydroxyretinoic acid also serves as a substrate for UDP-glucuronosyltransferase (s) and recombinant UGT2B7. 4-Hydroxyretinoic acid binds to the nuclear receptor RAR (Retinoic Acid Receptor), activates RAR and RXR-alpha, subsequently regulates gene expression and cell differentiation, and induces cancer cell apoptosis (Apoptosis). 4-Hydroxyretinoic acid also participates in multiple physiological processes such as immunoregulation, neuroprotection and antioxidation .
|
-
-
- HY-22024
-
|
5-OH-Flavone
|
Cytochrome P450
|
Others
|
|
5-Hydroxyflavone (5-OH-Flavone) is a flavonoid compound that undergoes oxidation-mediated conversion to 5,7-dihydroxyflavone and 5,6,7-trihydroxyflavone by human cytochrome P450 enzymes .
|
-
-
- HY-A0296
-
|
Clomethiazole hydrochloride
|
Cytochrome P450
|
Neurological Disease
|
|
Clomethiazole hydrochloride is a potent and orally active GABAA agonist . Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
|
-
-
- HY-B0854
-
-
-
- HY-N1050
-
|
|
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 .
|
-
-
- HY-B1036
-
|
|
Parasite
|
Infection
|
|
Decoquinate is an orally active, selective inhibitor of the mitochondrial bc1 complex, targeting Eimeria spp. sporozoites and first generation schizonts, and Plasmodium spp. Decoquinate inhibits electron transfer by competitively binding to the mitochondrial cytochrome b system, blocking the parasite's energy metabolism, thereby inhibiting its development and reproduction. Decoquinate has significant anticoccidial activity, preventing intestinal damage and improving host growth performance, and also has inhibitory effects on the liver and blood stages of Plasmodium. Decoquinate is mainly used in veterinary research to prevent and treat coccidiosis in ruminants and poultry .
|
-
-
- HY-17657
-
|
5-Androstenediol 3-sulfate sodium
|
Drug Intermediate
|
Metabolic Disease
|
|
Androst-5-enediol sulfate (5-Androstenediol 3-sulfate) sodium salt is an adrenal Δ5-steroid sulfate that synthesized by zona reticularis of adrenal depending on the lyase and Cytochrome b5 type A (CYB5A) activity. Androst-5-enediol sulfate sodium salt is a precursor hormone and can be desulfated to produce more potent androgens, including testosterone, in peripheral tissues like skin and liver. The serum level of Androst-5-enediol sulfate sodium salt has an age-related increase .
|
-
-
- HY-B2012
-
|
DPX-H6573
|
Environmental Pollutants
Fungal
|
Infection
|
|
Flusilazole (DPX-H6573) is a broad-spectrum fungicide and cytochrome P-450 inhibitor that can be used in studies related to fungal infections .
|
-
-
- HY-N7781
-
-
-
- HY-100386R
-
|
PCR 5332 (Standard)
|
Reference Standards
NTPDase
Cytochrome P450
|
Cardiovascular Disease
|
|
Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. 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 .
|
-
-
- HY-129491
-
|
CGP62221; O-Desmethyl PKC412
|
PKC
|
Cancer
|
|
O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo . Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
|
-
-
- HY-125348S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is one of the main metabolites of Paclitaxel (PTX) (HY-B0015), and it is generated by the liver cytochrome P450 enzyme CYP2C8. 6α-Hydroxy paclitaxel has bone marrow toxicity, but it can enhance the cytotoxicity of PTX against leukemia cells without causing cell toxicity. 6α-Hydroxy paclitaxel can be used in leukemia research.
|
-
-
- HY-B0476S
-
|
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 .
|
-
-
- HY-B0476R
-
|
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 .
|
-
-
- HY-113031
-
|
16α-Hydroxy-DHEA; 16α-OH-DHEA; 16α-hydroxy DHEA
|
Cytochrome P450
|
Endocrinology
|
|
16a-Hydroxydehydroisoandrosterone (16α-Hydroxy-DHEA) is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.
|
-
-
- HY-106547
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Rilmazafone (450191S) is an orally active sleep inducer. Rilmazafone targets cytochrome P-450b and cytochrome P-450e. Rilmazafone induces hepatic drug-metabolizing enzyme activity in rats, mice and dogs. Rilmazafone is applicable for insomnia-related research .
|
-
-
- HY-W700800
-
|
|
Cytochrome P450
|
Cancer
|
|
Flu-6 is a metabolite of Flutamide (HY-B0022). FLU-6 production in the liver requires the involvement of NADPH: cytochrome P450 reductase (CPR). Flutamide can inhibit prostate cancer progression .
|
-
-
- HY-B1351
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Bilberry Extract is a bilberry extract, and its components include: Anthocyanidins. Bilberry Extract has potential antioxidant activity and can regulate specific metabolic enzymes in the liver, such as cytochrome P450 (CYP) 2C11 and CYP2E1 involved in drug metabolism. .
|
-
-
- HY-N1431A
-
|
|
NOD-like Receptor (NLR)
Apoptosis
Cytochrome P450
NF-κB
PI3K
Akt
CDK
Caspase
Interleukin Related
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer .
|
-
-
- HY-N11546
-
|
|
Cytochrome P450
Bacterial
Fungal
|
Infection
Cancer
|
|
Sapindoside B is a substance with hepatoprotective activity, and also acts as a cytochrome P-450 (cytochrome P-450) inhibitor, antibacterial agent and membrane-disrupting agent. Sapindoside B reversibly inhibits the content of cytochrome P-450 in liver microsomes, suppresses the phenobarbital-induced increase in enzyme content, reduces the production of active metabolites mediated by cytochrome P-450, and alleviates hepatotoxic injury. Sapindoside B binds to Cutibacterium acnes lipase, reduces lipase activity, inhibits biofilm formation, and decreases bacterial adhesion. Sapindoside B exhibits cytotoxicity against human cancer, liver cancer, leukemia and glioblastoma cells. Sapindoside B inhibits mycelial growth of phytopathogenic fungal strains, possesses antibacterial activity against dermatophytes, and also has hemolytic/membrane-lytic activity. Sapindoside B can be used in research related to liver injury, Cutibacterium acnes biofilm-associated infections, gastric cancer, carcinoma, promyelocytic leukemia, glioblastoma, apple scab and grape gray mold .
|
-
-
- HY-118167
-
-
-
- HY-W099331
-
|
MEGX hydrochloride; Norlidocaine hydrochloride
|
Drug Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
Monoethylglycinexylidide (MEGX) hydrochloride is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver. Monoethylglycinexylidide has proven to be a highly sensitive indicator of hepatic dysfunction, especially in the field of liver transplantation .
|
-
-
- HY-B0476S1
-
|
|
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 .
|
-
-
- HY-150519
-
|
|
Factor XI
Kallikrein
|
Cardiovascular Disease
|
|
FXIa/Plasma kallikrein-IN-1 is an inhibitor of coagulation factor XIa (FXIa) and plasma kallikrein with Ki values of 187.70 nM and 151.6 nM, respectively. FXIa/Plasma kallikrein-IN-1 can be used in the research of thromboembolic diseases .
|
-
-
- HY-135739
-
-
-
- HY-N16478
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Echihumiline is an alkaloid targeting hepatic cytochrome P450 enzymes (CYP450). Echihumiline induces DNA cross-linking and oxidative stress in hepatocytes, leading to liver necrosis and fibrosis. Echihumiline is promising for research of liver diseases .
|
-
-
- HY-A0069A
-
|
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-A0069R
-
|
|
Reference Standards
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine succinate (Standard) is the analytical standard of Doxylamine succinate (HY-A0069). This product is intended for research and analytical applications. Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-N7454
-
|
|
Drug Metabolite
Bacterial
|
Infection
|
|
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
|
-
-
- HY-W762012
-
|
OCDD
|
Cytochrome P450
Environmental Pollutants
|
Others
|
|
Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant but is not acutely toxic. In rats, Octachlorodibenzo-p-dioxin (50 μg/kg i.v. or 50-5000 μg/kg p.o.) has a systemic elimination half-life of 3-5 months and accumulates and concentrates in the liver and adipose tissue after low-dose, repeated exposure. Repeated administration of octachlorodibenzo-p-dioxin causes increases in 7-ethoxyresorufin-O-deethylase (7-EROD) activity and total cytochrome P-450 levels .
|
-
-
- HY-B0885R
-
|
(±)-Econazol (Standard)
|
Reference Standards
Fungal
Bacterial
Calcium Channel
Cytochrome P450
|
Infection
Metabolic Disease
|
|
Econazole (Standard) ((±)-Econazol (Standard)) is the analytical standard of Econazole (HY-B0885). This product is intended for research and analytical applications. Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
|
-
-
- HY-B0822S1
-
|
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
|
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
-
- HY-N6972R
-
|
|
Autophagy
Reference Standards
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
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 .
|
-
-
- HY-N8094
-
|
|
Cytochrome P450
|
Others
|
|
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
|
-
- HY-121385
-
|
Ro 48-5033
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
|
-
- HY-118167R
-
|
|
Reference Standards
Drug Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
Monoethylglycinexylidide (Standard) is the analytical standard of Monoethylglycinexylidide. This product is intended for research and analytical applications. Monoethylglycinexylidide is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver .
|
-
- HY-W721249
-
-
- HY-B1311R
-
|
SKF-525A (Standard); U-5446 (Standard); RP-5171 (Standard)
|
Reference Standards
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .
|
-
- HY-137580
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
N-desmethyl Eletriptan is a metabolite of Eletriptan (HY-A0039). It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes.
|
-
- HY-145490
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
trans-hydroxy Glimepiride is an active metabolite of the sulfonylurea Glimepiride (HY-B0104). It is formed from glimepiride primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9.
|
-
- HY-116444A
-
|
|
Na+/K+ ATPase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
16-HETE is arachidonic acid metabolite through subterminal hydroxylation by cytochrome P-450. 16-HETE exhibits vasodilatory and PMN inhibitory effects and serves as biomarker for early stages of non-alcoholic fatty liver disease .
|
-
- HY-118788
-
-
- HY-129491S
-
|
CGP62221-d5; O-Desmethyl PKC412-d5
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism .
|
-
- HY-121385S
-
|
Ro 48-5033-d6
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
|
-
- HY-A0069AS
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine-d5 is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
|
-
- HY-160979
-
|
DA-5047
|
Histamine Receptor
|
Others
Endocrinology
|
|
Bisfentidine is an H2 receptor antagonist, Bisfentidine can block the H2 receptor on the cells of the stomach wall, and reduce the secretion of stomach acid. Bisfentidine binds to cytochrome P-450 in liver microsomes and affects drug metabolism. Bisfentidine can be used in the study of metabolic processes of drugs, lipid peroxidation processes and peptic ulcers diseases .
|
-
- HY-129105R
-
|
|
GABA Receptor
Cytochrome P450
Reference Standards
|
Neurological Disease
|
|
Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
|
-
- HY-A0069S
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine-d5 succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
|
-
- HY-135390
-
|
Ro 64-1056
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
|
-
- HY-W707708
-
|
|
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 .
|
-
- HY-113777
-
|
22-Hydroxy Docosahexaenoic acid; 22-OH DHA
|
Cytochrome P450
|
Metabolic Disease
|
|
22-HDHA (22-Hydroxy Docosahexaenoic acid) is an oxidation product of docosahexaenoic acid. In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
|
-
- HY-B0885S
-
|
(±)-Econazol-d6
|
Isotope-Labeled Compounds
Fungal
Bacterial
Calcium Channel
Cytochrome P450
|
Infection
Metabolic Disease
|
|
Econazole-d6 ((±)-Econazol-d6) is the deuterium labeled Econazole (HY-B0885). Econazole is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
|
-
- HY-169119
-
|
|
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 .
|
-
- HY-119694
-
|
|
Drug Metabolite
Mitochondrial Metabolism
Cytochrome P450
|
Cancer
|
|
Rotenolone is a metabolite of Rotenone (HY-B1756), inhibitor of Mitochondrial complex I, and antiproliferative agent, with an IC50 of 137 nM against bovine complex I. Rotenolone undergoes biotransformation via multiple cytochrome P450 isoenzymes in rainbow trout liver microsomes. Rotenolone exhibits anticancer activity against ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, and colon cancer. Rotenolone can be used in studies related to ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, and colon cancer .
|
-
- HY-100386S
-
|
PCR 5332-d4
|
Isotope-Labeled Compounds
NTPDase
Cytochrome P450
|
Cardiovascular Disease
|
|
Ticlopidine-d4 is the deuterium labeled Ticlopidine. 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 .
|
-
- HY-B0847S1
-
|
|
Fungal
Reactive Oxygen Species (ROS)
|
Infection
|
|
Propiconazole-d3 (nitrate) is the deuterium labeled Propiconazole nitrate. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
|
-
- HY-B0847S
-
|
|
Isotope-Labeled Compounds
Fungal
Reactive Oxygen Species (ROS)
|
Infection
|
|
Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 μM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 μg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS) .
|
-
- HY-W751181
-
|
CGP62221-13C6; O-Desmethyl PKC412-13C6
|
Isotope-Labeled Compounds
PKC
|
Cancer
|
|
O-Desmethyl midostaurin- 13C6 (CGP62221- 13C6; O-Desmethyl PKC412- 13C6) is the 13C-labeled O-Desmethyl Midostaurin (HY-129491). O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo . Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM.
|
-
- HY-B0153AS
-
|
|
Isotope-Labeled Compounds
NTPDase
Cytochrome P450
|
Cardiovascular Disease
|
|
Ticlopidine-d4 hydrochloride is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). 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 .
|
-
- HY-W707554
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cardiovascular Disease
|
|
Ticlopidine hydrochloride-d6 is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). 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 .
|
-
- HY-B0153AR
-
|
|
Reference Standards
NTPDase
Cytochrome P450
|
Cardiovascular Disease
|
|
Ticlopidine hydrochloride (Standard) is the analytical standard of Ticlopidine hydrochloride (HY-B0153A). This product is intended for research and analytical applications. 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 .
|
-
- HY-W778179
-
|
LRCL 3794-13C,d3
|
Isotope-Labeled Compounds
COX
Cytochrome P450
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
|
Benoxaprofen- 13C, d3 is the 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms .
|
-
- HY-13568R
-
|
LRCL 3794 (Standard)
|
Reference Standards
COX
Cytochrome P450
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
|
Benoxaprofen (Standard) is the analytical standard of Benoxaprofen. This product is intended for research and analytical applications. Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms .
|
-
- HY-114625
-
|
|
Parasite
Mitochondrial Metabolism
|
Infection
|
|
Amquinate is a coccidiostat and a cytochrome b inhibitor. Amquinate blocks cytochrome-mediated electron transport near cytochrome b in mitochondria, acting downstream of coenzyme Q without affecting succinate dehydrogenase or NADH dehydrogenase. Amquinate inhibits succinate- and malate plus pyruvate-supported mitochondrial respiration in Eimeria tenella and does not affect L-ascorbate-supported respiration or any mitochondrial respiration in chicken liver mitochondria. Amquinate exhibits selective anticoccidial activity against wild-type Eimeria tenella. Amquinate can be used for the research of coccidiosis (Eimeria tenella infection) .
|
-
- HY-P11489
-
|
|
Cyclophilin
Reactive Oxygen Species (ROS)
NF-κB
Caspase
Apoptosis
|
Metabolic Disease
|
|
RN-0001 is a cyclophilin (Cyp) inhibitor with Ki values of 4.1 nM and 12.0 nM against CypA and CypD, respectively, and an EC50 of 916 nM for CypD. RN-0001 binds directly to CypD, inhibits the peptidyl-prolyl cis-trans isomerase activities of CypD and CypA, and prevents CypD-dependent mitochondrial permeability transition pore opening. RN-0001 improves mitochondrial function, reduces ROS production, inhibits the expression of lipogenic markers, blocks the nuclear translocation of NF-κB p65, and decreases the release of activated caspase-3 and cytochrome c. RN-0001 can be used in the research of alcohol-associated liver disease .
|
-
- HY-121385S1
-
|
Ro 48-5033-d4
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
|
-
- HY-W009659
-
|
|
Drug Intermediate
|
Others
|
|
m-Terphenyl is a non-chlorinated trisphenyl compound and is commonly used as the basic structure for industrial raw materials (such as plastic additives). In liver enzyme induction experiments, m-Terphenyl exhibits weak activity and is unable to significantly activate the cytochrome P-450-dependent monooxygenase system .
|
-
- HY-B0476S3
-
-
- HY-166530S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cardiovascular Disease
|
|
Ticlopidine-d6 hydrochloride is the deuterium labeled Ticlopidine hydrochloride. 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 .
|
-
- HY-182637
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
ACT-774312 is a potent and selective CRTH2 antagonist with an IC50 of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD2-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.
|
-
- HY-181644
-
|
|
MetAP
|
Infection
|
|
NS-181 is an orally active MetAP2 inhibitor and antiamebic agent with oral effectiveness.NS-181 functionally inhibits methionine aminopeptidase 2, a protein critical for Entamoeba histolytica proliferation. NS-181 exerts antiamebic activity against Entamoeba histolytica, leading to resolution of amebic liver abscess. NS-181 can be used for the research of amebiasis .
|
-
- HY-182358
-
|
|
Apoptosis
|
Cancer
|
|
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research .
|
-
- HY-183317
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Interleukin Related
Apoptosis
Caspase
PARP
|
Cancer
|
|
IDO1-IN-34 is a selective IDO1 inhibitor with an IC50 of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia .
|
-
- HY-103084
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
PDE5-IN-1 is an orally active, selective PDE5 inhibitor with an IC50 of 5.6 nM. PDE5-IN-1 forms hydrogen bond interactions with the Q817 residue in the catalytic domain of PDE5, and aromatic π-π stacking interactions with the F820 residue. PDE5-IN-1 exerts anti-cardiac hypertrophy and vasodilatory effects, reduces mean pulmonary arterial pressure and right ventricular hypertrophy index. PDE5-IN-1 can be used in the research of pulmonary arterial hypertension .
|
-
- HY-N11846
-
|
|
Apoptosis
Caspase
|
Inflammation/Immunology
Cancer
|
|
4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases .
|
-
- HY-181643
-
|
|
MetAP
|
Infection
|
|
YOK24 is an orally active MetAP2 inhibitor and anti-amoebic agent. YOK24 binds covalently to MetAP2 and inhibits its peptidase activity, where MetAP2 is a protein essential for the proliferation of *Entamoeba histolytica*. YOK24 can be used in the research of amoebiasis .
|
-
- HY-W714300
-
|
|
Fungal
|
Infection
|
|
Nuarimol is a fungicide used for plant protection in agriculture. Nuarimol is a phenobarbital-type inducer of hepatic drug-metabolizing enzymes. It triggers transient but robust regenerative hepatocyte proliferation accompanied by hepatomegaly by causing reversible hepatocellular injury .
|
-
- HY-183606
-
|
|
Bacterial
|
Infection
|
|
Mycobacterium tuberculosis-IN-9 is an orally active Mycobacterium tuberculosis BioA inhibitor with a Ki value of 0.2 nM. Mycobacterium tuberculosis-IN-9 targets the biotin biosynthesis pathway. Mycobacterium tuberculosis-IN-9 inhibits the growth of Mycobacterium tuberculosis in mouse models and is effective against both drug-sensitive and drug-resistant strains. Mycobacterium tuberculosis-IN-9 can be used for the research of tuberculosis .
|
-
- HY-181932
-
|
|
MAP4K
|
Cancer
|
|
HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer .
|
-
- HY-181779
-
|
|
Bacterial
|
Infection
|
|
Pyridomycin-4-F, Pyridomycin (HY-111402) derivative, is an antimycobacterial agent targeting fatty acid synthesis enzyme InhA (enoyl ACP reductase). Pyridomycin-4-F binds to the pyridomycin binding pocket of InhA, forms hydrogen bond interactions with Lys-165. Pyridomycin-4-F can be used for the research of tuberculosis .
|
-
- HY-131453
-
|
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Mitochondrial respiration-IN-1 is a mitochondrial respiratory inhibitor. Mitochondrial respiration-IN-1 reduces platelet aggregation, adhesion, and platelet-induced coagulation responses. Mitochondrial respiration-IN-1 induces adaptive glycolysis, decreases mitochondrial membrane potential, selectively reduces ATP production derived from oxidative phosphorylation, and exerts bidirectional regulatory effects on cell proliferation. Mitochondrial respiration-IN-1 activates UPRmt and upregulates the expression of SDHA-1 and MT-CO1. Mitochondrial respiration-IN-1 restores metabolic homeostasis in type 2 diabetic mice. Mitochondrial respiration-IN-1 can be used to investigate diseases mediated by inappropriate platelet activation/aggregation and type 2 diabetes .
|
-
- HY-N9858
-
|
|
CXCR
Wnt
β-catenin
|
Metabolic Disease
|
|
Herpetin is an active lignan. Herpetin acts as a bone marrow mesenchymal stem cell inducer that activates the SDF-1/CXCR4 axis and the Wnt/β-catenin pathway. Herpetin is applicable to research related to acute liver injury .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P11489
-
|
|
Cyclophilin
Reactive Oxygen Species (ROS)
NF-κB
Caspase
Apoptosis
|
Metabolic Disease
|
|
RN-0001 is a cyclophilin (Cyp) inhibitor with Ki values of 4.1 nM and 12.0 nM against CypA and CypD, respectively, and an EC50 of 916 nM for CypD. RN-0001 binds directly to CypD, inhibits the peptidyl-prolyl cis-trans isomerase activities of CypD and CypA, and prevents CypD-dependent mitochondrial permeability transition pore opening. RN-0001 improves mitochondrial function, reduces ROS production, inhibits the expression of lipogenic markers, blocks the nuclear translocation of NF-κB p65, and decreases the release of activated caspase-3 and cytochrome c. RN-0001 can be used in the research of alcohol-associated liver disease .
|
-
- HY-K6304
-
|
|
|
MCE Human iPSC/ESC Hepatocyte Induction Differentiation Kit enables the efficient generation of hepatocyte-like cells with a high degree of maturation within 21 d. The resulting cells stably express multiple key hepatic functional markers, including albumin (ALB), cytochrome P450 (CYP) family enzymes, and other liver-specific functional molecules, and exhibit typical hepatocellular phenotypes and functions.
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N6972
-
-
-
- HY-N2181
-
|
|
Quinones
Classification of Application Fields
Phenols
Polyphenols
Plants
Lithospermum erythrorhizon Sieb. et Zucc.
Naphthalene Quinones
Boraginaceae
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Cytochrome P450
Apoptosis
Bacterial
Autophagy
|
|
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD) .
|
-
-
- HY-N1431
-
|
|
Apocynaceae
Alkaloids
Structural Classification
Plants
Indole Alkaloids
Catharanthus roseus (L.) G. Don
Source Classification
|
NOD-like Receptor (NLR)
Apoptosis
Cytochrome P450
NF-κB
PI3K
Akt
CDK
Caspase
Interleukin Related
p38 MAPK
|
|
Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer .
|
-
-
- HY-N5132
-
|
|
Structural Classification
Other Monoterpenes
Classification of Application Fields
Terpenoids
Other Diseases
Umbelliferae
Plants
Vernonia Schreb.
Disease Research Fields
Source Classification
|
Cytochrome P450
|
|
(-)-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 .
|
-
-
- HY-22024
-
-
-
- HY-N1050
-
|
|
Terpenoids
Sesquiterpenes
Plants
Curcuma elata Roxb.
Source Classification
Zingiberaceae
|
mTOR
Ribosomal S6 Kinase (RSK)
Bacterial
|
|
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 .
|
-
-
- HY-17657
-
|
5-Androstenediol 3-sulfate sodium
|
Structural Classification
Endogenous metabolite
Steroids
Source Classification
|
Drug Intermediate
|
|
Androst-5-enediol sulfate (5-Androstenediol 3-sulfate) sodium salt is an adrenal Δ5-steroid sulfate that synthesized by zona reticularis of adrenal depending on the lyase and Cytochrome b5 type A (CYB5A) activity. Androst-5-enediol sulfate sodium salt is a precursor hormone and can be desulfated to produce more potent androgens, including testosterone, in peripheral tissues like skin and liver. The serum level of Androst-5-enediol sulfate sodium salt has an age-related increase .
|
-
-
- HY-N7781
-
-
-
- HY-N1431A
-
|
|
Apocynaceae
Alkaloids
Plants
Indole Alkaloids
Catharanthus roseus (L.) G. Don
Source Classification
|
NOD-like Receptor (NLR)
Apoptosis
Cytochrome P450
NF-κB
PI3K
Akt
CDK
Caspase
Interleukin Related
p38 MAPK
|
|
Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer .
|
-
-
- HY-N11546
-
|
|
Structural Classification
Eleutherococcus sieboldianus Makino
Terpenoids
Diterpenoids
Plants
Araliaceae
Source Classification
|
Cytochrome P450
Bacterial
Fungal
|
|
Sapindoside B is a substance with hepatoprotective activity, and also acts as a cytochrome P-450 (cytochrome P-450) inhibitor, antibacterial agent and membrane-disrupting agent. Sapindoside B reversibly inhibits the content of cytochrome P-450 in liver microsomes, suppresses the phenobarbital-induced increase in enzyme content, reduces the production of active metabolites mediated by cytochrome P-450, and alleviates hepatotoxic injury. Sapindoside B binds to Cutibacterium acnes lipase, reduces lipase activity, inhibits biofilm formation, and decreases bacterial adhesion. Sapindoside B exhibits cytotoxicity against human cancer, liver cancer, leukemia and glioblastoma cells. Sapindoside B inhibits mycelial growth of phytopathogenic fungal strains, possesses antibacterial activity against dermatophytes, and also has hemolytic/membrane-lytic activity. Sapindoside B can be used in research related to liver injury, Cutibacterium acnes biofilm-associated infections, gastric cancer, carcinoma, promyelocytic leukemia, glioblastoma, apple scab and grape gray mold .
|
-
-
- HY-N16478
-
-
-
- HY-N7454
-
-
-
- HY-N6972R
-
|
|
Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
|
Autophagy
Reference Standards
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
|
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 .
|
-
-
- HY-N8094
-
-
-
- HY-121385
-
-
-
- HY-114625
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Parasite
Mitochondrial Metabolism
|
|
Amquinate is a coccidiostat and a cytochrome b inhibitor. Amquinate blocks cytochrome-mediated electron transport near cytochrome b in mitochondria, acting downstream of coenzyme Q without affecting succinate dehydrogenase or NADH dehydrogenase. Amquinate inhibits succinate- and malate plus pyruvate-supported mitochondrial respiration in Eimeria tenella and does not affect L-ascorbate-supported respiration or any mitochondrial respiration in chicken liver mitochondria. Amquinate exhibits selective anticoccidial activity against wild-type Eimeria tenella. Amquinate can be used for the research of coccidiosis (Eimeria tenella infection) .
|
-
-
- HY-N11846
-
|
|
Structural Classification
Natural Products
Glycyrrhiza glabra Linn.
Leguminosae
Plants
Source Classification
|
Apoptosis
Caspase
|
|
4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases .
|
-
-
- HY-N9858
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-125348S
-
|
|
|
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is one of the main metabolites of Paclitaxel (PTX) (HY-B0015), and it is generated by the liver cytochrome P450 enzyme CYP2C8. 6α-Hydroxy paclitaxel has bone marrow toxicity, but it can enhance the cytotoxicity of PTX against leukemia cells without causing cell toxicity. 6α-Hydroxy paclitaxel can be used in leukemia research.
|
-
-
- HY-B0476S
-
|
|
|
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 .
|
-
-
- HY-B0476S1
-
|
|
|
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 .
|
-
-
- HY-B0822S1
-
|
|
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
-
- HY-129491S
-
|
|
|
O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism .
|
-
-
- HY-121385S
-
|
|
|
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
|
-
-
- HY-A0069AS
-
|
|
|
Doxylamine-d5 is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-A0069S
-
|
|
|
Doxylamine-d5 succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-W707708
-
|
|
|
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 .
|
-
-
- HY-B0885S
-
|
|
|
Econazole-d6 ((±)-Econazol-d6) is the deuterium labeled Econazole (HY-B0885). Econazole is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
|
-
-
- HY-100386S
-
|
|
|
Ticlopidine-d4 is the deuterium labeled Ticlopidine. 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 .
|
-
-
- HY-B0847S1
-
|
|
|
Propiconazole-d3 (nitrate) is the deuterium labeled Propiconazole nitrate. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
|
-
-
- HY-B0847S
-
|
|
|
Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 μM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 μg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS) .
|
-
-
- HY-W751181
-
|
|
|
O-Desmethyl midostaurin- 13C6 (CGP62221- 13C6; O-Desmethyl PKC412- 13C6) is the 13C-labeled O-Desmethyl Midostaurin (HY-129491). O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo . Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM.
|
-
-
- HY-B0153AS
-
|
|
|
Ticlopidine-d4 hydrochloride is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). 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 .
|
-
-
- HY-W707554
-
|
|
|
Ticlopidine hydrochloride-d6 is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). 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 .
|
-
-
- HY-W778179
-
|
|
|
Benoxaprofen- 13C, d3 is the 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms .
|
-
-
- HY-121385S1
-
|
|
|
Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
|
-
-
- HY-B0476S3
-
|
|
|
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 .
|
-
-
- HY-166530S
-
|
|
|
Ticlopidine-d6 hydrochloride is the deuterium labeled Ticlopidine hydrochloride. 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 .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: