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カタログ番号 | 製品名 | 別名 | ターゲット |
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T64037 | CYP3A4-IN-2 | ||
CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.055 μM). CYP3A4-IN-2 is a ritonavir analogue with a more hydrophobic R2 side group and stronger inhibition than ritonavir. CYP3A4-IN-2 is capab... | |||
T64032 | CYP3A4-IN-3 | ||
CYP3A4-IN-3 is a specific, highly affinity cytochrome P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) inhibitor (IC50: 0.075 μM). CYP3A4-IN-3 is an analogue of ritonavir with a simpler structure and twice as much inhibi... | |||
T63954 | CYP3A4-IN-1 | ||
CYP3A4-IN-1 is a potent inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.085 μM). | |||
T20626 | Esomeprazole | Proton pump , Cysteine Protease | |
Esomeprazole is the S-isomer of omeprazole, inhibits the lysosomal cysteine protease legumain to prevent cancer metastasis. Esomeprazole is a proton pump inhibitors (PPI). | |||
T10423 | AWZ1066S | Parasite | |
AWZ1066S is a highly specific anti-Wolbachia drug candidate for the short-course treatment of filariasis (EC50: 2.5 nM in cell assay). | |||
T28827 | Sofpironium bromide | BBI4000,BBI 4000,BBI-4000 | Others , AChR |
Sofpironium bromide (BBI4000) belongs to a class of drugs called anticholinergics, which exert their effect by blocking the action of acetylcholine. | |||
T4697 | ABBV-744 | ABBV744 | Epigenetic Reader Domain , HIV Protease |
ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS. | |||
T9054 | RO6889678 | HBV | |
RO6889678 is HBV inhibitor with a complex ADME profile. | |||
T2397 | Topiroxostat | FYX-051 | P450 , ROS , Xanthine Oxidase |
Topiroxostat (FYX-051) is a selective xanthine oxidase inhibitor developed for treatment and management of hyperuricemia and gout. | |||
T1434 | Clarithromycin | A-56268 | P450 , ribosome , MRP , Antibacterial , Antibiotic , Autophagy |
Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classif... | |||
T6150 | TAK-715 | p38 MAPK , Casein Kinase , JNK | |
TAK-715 is a p38 MAPK inhibitor for p38α. | |||
T2686L | Esomeprazole Sodium | (S)-Omeprazole sodium | ATPase , Proton pump |
Esomeprazole Sodium ((S)-Omeprazole sodium) is the S-isomer of omeprazole with selective and irreversible proton pump inhibitor activity.Esomeprazole acts as an exosome inhibitor by blocking the exosome release via the i... | |||
T21404 | Fluticasone furoate | Veramyst,Allermist,Avamys,Fluticasone furoate | Glucocorticoid Receptor |
Fluticasone furoate (Avamys) is a synthetic trifluorinated corticosteroid derived from fluticasone with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflammatory, anti-asthmatic activity, and low systemic exposure... | |||
T1290 | Oxiconazole nitrate | Ro 13-8996 | Others , Antibiotic , Antifection , Antifungal |
Oxiconazole nitrate (Ro 13-8996) is the nitrate salt form of oxiconazole, a broad spectrum imidazole derivative with antifungal activity. Although the exact mechanism of action has yet to be fully elucidated, oxiconazole... | |||
T10989 | Dehydroaripiprazole | OPC-14857,DM-14857 | 5-HT Receptor |
Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has anti... | |||
T12146 | N-Desmethyl-Apalutamide | N-Desmethyl Apalutamide | P450 , Androgen Receptor |
N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite. | |||
T20656 | Verapamil | NSC 135784,NSC-135784,CP-16533-1,(±)-Verapamil | P450 , Calcium Channel , P-gp |
Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias... | |||
T1010 | Verapamil hydrochloride | Manidon,(±)-Verapamil hydrochlorid,Verapamil HCl,Calcan hydrochloride | P450 , Calcium Channel , P-gp |
Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent. | |||
T77698 | HCYP3A4 Fluorogenic substrate 1 | Others | |
hCYP3A4 Fluorogenic substrate 1 is a phthalimide derivative and shows low activity against COX. | |||
T79343 | HCYP3A4-IN-1 | ||
hCYP3A4-IN-1 (compound C6) is a potent, orally active inhibitor of hCYP3A4, exhibiting IC50 values of 43.93 nM in human liver microsomes (HLMs) and 153.00 nM in the CHO-3A4 stably transfected cell line. It competitively ... | |||
T4498 | Stiripentol | BCX2600,Diacomit | P450 |
Stiripentol (BCX2600) (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.516 μM and IC50 of 1.58/3.29 μM... | |||
T21548 | PF-4981517 | CYP3cide | P450 |
PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. P... | |||
T0679 | Ketoconazole | R-41400,Xolegel,(±)-Ketoconazol,Extina | NADPH-oxidase , P450 , Hydroxylase , Antifungal , Ras |
Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent. | |||
T7618 | Pyributicarb | TSH-888 | P450 |
Pyributicarb (TSH-888) is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR). | |||
T37149 | Carbamazepine 10,11-epoxide | Others | |
Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine.1,2It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells e... | |||
T19526 | Pradefovir mesylate | Pradefovir mesilate,Remofovir mesylate,Hepavir B | P450 |
Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM. | |||
T15641 | K777 | APC-3316 | P450 , Cysteine Protease , CCR |
K777 is a potent, orally active and irreversible inhibitor of cysteine protease. K777 is a potent CYP3A4 inhibitor (IC50= 60 nM). K777 is also a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 ... | |||
T60009 | YS-370 | P-gp | |
YS-370 is an orally active inhibitor of P-gp and shows moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance to paclitaxel and colchicine and exhibits stronger antitumor activity in combina... | |||
T6050 | TAK-700 | (S/R)-Orteronel,Orteronel | P450 |
TAK-700 (Orteronel) (Orteronel) is a potent and highly selective human 17, 20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3. | |||
T9043 | AS1810722 | P450 , STAT | |
AS1810722, a fused bicyclic pyrimidine derivative, is an orally active and potent inhibitor of STAT6, demonstrating an IC50 of 1.9 nM. It exhibits effective inhibition of CYP3A4, positioning it as a promising candidate f... | |||
T63208 | Aβ-IN-1 | Gamma-secretase | |
Aβ-IN-1 is a novel, potent and orally active γ-secretase modulator (GSM). Aβ-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ-IN-1 shows a sustained pharma... | |||
T3724 | Rolapitant hydrochloride | Rolapitant HCl | Neurokinin receptor |
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CY... | |||
T36665 | Dehydro Nifedipine | BAY-b 4759 | |
Dehydro Nifedipine (BAY-b 4759) is the main metabolite of nifedipine in human plasma. Dehydro Nifedipine inhibits glucose uptake in PC-12 cells with an IC50 value of 130 μM. Nifedipine is a calcium channel blocker used i... | |||
T1266 | Terfenadine | (±)-Terfenadine,MDL-991 | Apoptosis , Potassium Channel , 5-HT Receptor , Caspase , Na+/Ca2+ Exchanger , HER , AChR , Histamine Receptor |
Terfenadine ((±)-Terfenadine) is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistaminic and non-sedative effects. | |||
T6260 | AMG-208 | AMG 208 | P450 , c-Met/HGFR |
AMG-208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1. | |||
T12171 | Nampt-IN-5 | P450 , NAMPT | |
Nampt-IN-5 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) . | |||
T7699 | AZD7325 | AZD-7325 | P450 , GABA Receptor |
AZD7325 (AZD-7325) is a GABA-Aα2,3 -selective receptor modulator. | |||
T4567 | Sulfaphenazole | Plisulfan,Raziosulfa,Depocid,Depotsulfonamide | P450 , Antibacterial |
Sulfaphenazole (Plisulfan) is an inhibitor of CYP2C9 (Ki: 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 μM for CYP2C8/CYP2C18, respectively, and no activity at CYP1A1, CYP1... | |||
T0100L | Atazanavir | Zrivada,Reyataz,Latazanavir,BMS-232632 | P450 , SARS-CoV , HIV Protease , P-gp |
Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor. | |||
T1149 | Fenofibrate | Procetofen,Lipanthyl,Lipantil | P450 , PPAR , Autophagy |
Fenofibrate (Lipanthyl) is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity. | |||
T1561 | Clobetasol propionate | Dermovate,Clobetasol 17-propionate,CGP9555,Temovate,CCl 4725 | Glucocorticoid Receptor , P450 |
Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain a... | |||
T4190 | Ticlopidine | PCR 5332,Ticlid | ATPase , Adiponectin receptor |
Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor. | |||
T4488 | GSK-25 | GSK25 | ROCK , S6 Kinase , mTOR |
GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested). | |||
T2305 | Isavuconazole | BAL-4815,RO-0094815 | P450 , Antibiotic , Antifungal |
Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabr... | |||
T11964 | MCH-1 antagonist 1 | P450 | |
T14678 | BMS-819881 | P450 | |
T22254 | Alflutinib | AST2818,ASK120067 | EGFR , P450 |
Alflutinib (ASK120067) is an inhibitor of EGFR, and its targets including EGFR activating mutations and T790M, thus leading to tumor growth inhibition. | |||
T25823 | ML368 | SR9186,ML 368,SR-9186,SR 9186,ML-368 | |
ML368 is a selective inhibitor of CYP3A4. | |||
T30093 | AP-24567 | ||
AP-24567 is a CYP3A4-mediated metabolite. | |||
T38911 | Nav1.7-IN-8 | Nav1.7-IN-8 | |
Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP... |
カタログ番号 | 製品名 | 別名 | ターゲット |
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T10835 | Cletoquine | Desethylhydroxychloroquine | Parasite , Antifection |
Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatme... | |||
T3797 | Isosilybin | Isosilybinin,Isosilibinin,Silymarin,Silybin B,Q-100795 | P450 |
Isosilybin (Isosilibinin) and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients. | |||
T2S1434 | Bergaptol | 5-Hydroxyfuranocoumarin,4-Hydroxybergapten,5-Hydroxypsoralen | P450 |
1. Bergaptol (4-Hydroxybergapten) shows very good radical scavenging activity. 2. Bergaptol is a potent inhibitor of debenzylation activity of CYP3A4 enzyme. | |||
T5594 | Cedrol | P450 , Antifungal | |
Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively) | |||
T3401 | Ginsenoside F1 | 20(S)-Ginsenoside F1 | P450 , Endogenous Metabolite |
Ginsenoside F1 (20(S)-Ginsenoside F1) is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of the activity of CYP2D6. | |||
T11218 | ε-Viniferin | epsilon-Viniferin | P450 |
ε-Viniferin (epsilon-Viniferin) a dimer of resveratrol, shows the inhibitory effects of epsilon-viniferin on human CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2B6, CYP2E1, CYP3A4 and CYP4A activities. | |||
T3411 | Curdione | (+)-Curdione | P450 |
Curdione ((+)-Curdione) inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be a candidate for anti-inflammatory and Y chemo... | |||
TN1650 | Friedelin | P450 , NOS , Caspase , Prostaglandin Receptor | |
Friedelin possesses antioxidant, gastroprotective, anti-diarrhoeal, liver protective, anti-inflammatory, analgesic and antipyretic activities. | |||
T3417 | Amentoflavone | Didemethyl-ginkgetin,Amenthoflavone,3',8''-Biapigenin | Apoptosis , P450 , Phospholipase , Reactive Oxygen Species , Opioid Receptor , COX , Antibacterial , RSV , Antifungal |
Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhib... | |||
T2878 | Ginsenoside Rd | Panaxoside Rd,Sanchinoside Rd,Gypenoside VIII | P450 , Calcium Channel , NF-κB , COX , Endogenous Metabolite |
Ginsenoside Rd (Gypenoside VIII) may have properties that inhibit or prevent the growth of tumors. | |||
T3002 | Piperine | 1-Piperoylpiperidine,Bioperine | P450 , Endogenous Metabolite , P-gp , Autophagy |
Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders. | |||
T3669 | Curcumenol | (+)-Curcumenol | P450 |
Curcumenol ((+)-Curcumenol), one of the major components of Zedoary turmeric oil, is an antibiotic drug which has anti-Y, anti-inflammation activity. Curcumenol may be safely used without inducing metabolic drug-drug int... | |||
T3735 | Tetrahydrocurcumin | Sabiwhite,Tetrahydrodiferuloylmethane,HZIV 81-2,Tetrahydro Curcumin | P450 , Endogenous Metabolite , Autophagy |
Tetrahydrocurcumin (HZIV 81-2), a major metabolite of curcumin, has strong antioxidant and cardioprotective properties. | |||
T4A2458 | Resibufogenin | Bufogenin,Recibufogenin | Others |
1. Resibufogenin (Bufogenin) is a cytotoxic steroid isolated from the Chinese drug ChanSu. 2. Resibufogenin can inhibit rectifier potassium current ( I K ) and transient potassium current ( I A ), it has pathological eff... | |||
T5S1097 | Neferine | (R)-1,2-Dimethoxyaporphine,(-)-Neferine | Apoptosis , NF-κB , Autophagy |
1. Neferine ((-)-Neferine) has anti-tumor activities , Metabolic activation mediated by CYP3A4 and GSH depletion enhanced Neferine-induced cytotoxicity. 2. Neferine can be helpful to increase the efficacy of DOX and to a... | |||
T7056 | Dronedarone | SR 33589 | P450 , Potassium Channel , Calcium Channel , Sodium Channel , Adrenergic Receptor , AChR , Autophagy |
Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation. | |||
T1011 | Itraconazole | R51211 | P450 , Hedgehog/Smoothened , Antibiotic , Autophagy , Antifungal |
Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis. | |||
T2946 | Tanshinone IIA sulfonate sodium | Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium | CaMK , P450 , Calcium Channel |
Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor... | |||
TN1343 | 8-Geranyloxypsoralen | Anti-infection , P450 , BACE | |
8-Geranyloxypsoralen inhibits α2-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat arterial tissues. 8-Geranyloxypsoralen possesses nematicidal act... | |||
TN3147 | 6',7'-Dihydroxybergamottin | P450 | |
6',7'-Dihydroxybergamottin(DHB), a well-known inhibitor of CYP3A4, the inhibition of CYP3A4 activity by DHB includes the inhibition of POR activity, DHB can inhibit nifedipine oxidation in a concentration-dependent manne... | |||
T82556 | Dihydrocubebin | (-)-Dihydrocubebin | |
Dihydrocubebin, isolated from Piper cubeba, serves as a potent and selective inhibitor of cytochrome P450 3A4 (CYP3A4) [1]. | |||
T4S1421 | Praeruptorin B | Praeruptorin D | NPC1L1 , Fatty Acid Synthase |
Praeruptorin B is an inhibitor of sterol regulatory element-binding proteins (SREBPs). It can also significantly up-regulate CYP3A4 expression and activity via the PXR-mediated pathway. | |||
TN2144 | Resveratroloside | P450 , NO Synthase | |
Resveratroloside has cardioprotective effect, it exhibits α±-glucosidase inhibitory activity, it also can inhibit hydroxylation of testosterone by CYP3A4. | |||
T37810 | 6',7'-Epoxybergamottin | ||
6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, a... | |||
TN1843 | Kushenol K | PDE , HSV | |
Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K shows weak antiviral activity against Herpes simplex virus t... | |||
TN1378 | α-Viniferin | ALPHA-VINIFERIN | P450 , NO Synthase , Prostaglandin Receptor |
α-Viniferin known as 2-arylbenzofuran flavonoids, that are inhibitors of prostaglandin H2 synthetase. α-Viniferin has anti-Alzheimer's disease, anti-tuberculosis, anti-tumor, anti-inflammation, anti-diabetes and other ph... |
カタログ番号 | 製品名 | Species | Expression System |
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TMPY-05321 | CYP3A4 Protein, Human, Recombinant (His) | Human | E. coli |
CYP3A4 is an important member of the cytochrome P450 enzyme superfamily, with 33 allelic variants. Human cytochrome P450 3A4 (CYP3A4) is an important drug metabolizing enzyme involved in a number of drug-drug and food-dr... | |||
TMPH-01259 | AMFR Protein, Human, Recombinant (His) | Human | E. coli |
E3 ubiquitin-protein ligase that mediates the polyubiquitination of lysine and cysteine residues on target proteins, such as CD3D, CYP3A4, CFTR, INSIG1, SOAT2/ACAT2 and APOB for proteasomal degradation. Component of a VC... | |||
TMPH-01260 | AMFR Protein, Human, Recombinant (hFc) | Human | HEK293 Cells |
E3 ubiquitin-protein ligase that mediates the polyubiquitination of lysine and cysteine residues on target proteins, such as CD3D, CYP3A4, CFTR, INSIG1, SOAT2/ACAT2 and APOB for proteasomal degradation. Component of a VC... |