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カタログ番号 | 製品名 | 別名 | ターゲット |
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T12490 | Pitavastatin lactone | Others | |
Pitavastatin lactone is a major Pitavastatin metabolite in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes. | |||
T6031 | GNE0877 | GNE 0877,GNE-0877 | LRRK2 |
GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM). | |||
T6714 | URB-597 | KDS-4103,FAAH Inhibitor II | Mitophagy , FAAH , Autophagy |
URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets. | |||
T3424 | Ezutromid | BMN 195,VOX-C1100,SMT C1100 | Others |
Ezutromid (BMN 195) is a translation modulator of Small utrophin (EC50: 0.4 uM). Ezutromid is an orally bioavailable small molecule that transcriptionally upregulates the utrophin gene, increasing both utrophin mRNA and ... | |||
T13373 | YM17E | Acyltransferase , AChR | |
T20373 | 1-Phenylpyrrole | NSC16581,NSC-16581,NSC 16581 | Others |
1-Phenylpyrrole (NSC-16581) is an inhibitor of CYP450 dependant monooxygenase activity in microsomes from rat liver. | |||
T22148 | (S)-Lisofylline | Others | |
(S)-Lisofylline is the inactive optical enantiomer of (R)-lisofylline which is an anti-inflammatory agent. (S)-Lisofylline is exclusively converted to pentoxifylline in human liver microsomes. | |||
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. | |||
T73040 | CYP1B1-IN-4 | P450 | |
CYP1B1-IN-4, a 2,4-diarylthiazole compound, exhibits selective inhibition of CYP1B1 (IC50=0.2 nM), demonstrating minimal cytotoxicity and high stability in human and rat liver microsomes [1]. | |||
T11235 | Estradiol 3-sulfamate | E2MATE,BLE 00084,ES-J 995 | Estrogen Receptor/ERR |
Estradiol 3-sulfamate (BLE 00084) is an orally active and highly potent steroidal estrone sulfatase (ES) inhibitor.Estradiol 3-sulfamate has a K(i) value of 73 nM for ES in human placental microsomes and can be used in t... | |||
T11339 | Furegrelate sodium | U-63557A | PPAR |
T27918 | LY 43578 | LY-43578,LY43578 | P450 , Aromatase |
LY 43578 is an orally active aromatase inhibitor. LY43578 could inhibit O-demethylation of P-450-dependent p-nitroanisole and N-demethylation of ethylmorphine (IC50 of 0.3 and 5 μm, respectively) in rat liver microsomes.... | |||
T14983 | Clomethiazole | Distraneurin,Chlormethiazole,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE | P450 , GABA Receptor |
Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: C... | |||
T27371 | FR-167356 | FR167356,FR 167356 | ATPase |
FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces b... | |||
T3647 | HTHQ | HX 1171,HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone),1-O-hexyl-2,3,5-trimethylhydroquinone | Reactive Oxygen Species |
HTHQ (HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone)), a hydroquinone monoalkyl ether, is an effective anti-oxidative agent. HTHQ is a potent anti-lipid-peroxidative compound and its antioxidation activity to be extremely e... | |||
T14953 | Chloroquinoxaline sulfonamide | Chloroquinoxaline,NSC-339004 | Antibiotic |
Chloroquinoxaline sulfonamide (Chloroquinoxaline) is a structural analog of sulfaquinoxaline, an organic micropollutant that is frequently detected at low levels in drinking water and surface water.Chloroquinoxaline sulf... | |||
T21254 | Vonoprazan Fumarate | TAK-438,TAK 438,Vonoprazan Fumurate,TAK438 | Proton pump |
Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19... | |||
T28449 | Pradefovir | ICN-2001-3,MB-6866,ICN-20013,MB-06866,Remofovir | HBV |
Pradefovir (Remofovir) is a reverse transcriptase inhibitor potentially for treatment of chronic HBV infection. Pradefovir is also a liver-targeted prodrug of adefovir. After metabolic activation, Pradefovir was converte... | |||
T23549 | YM 511 | P450 , Aromatase | |
YM 511 is a highly specific non-steroidal aromatase inhibitor. YM 511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM 511 slightly ... | |||
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... | |||
T27061 | CP-24879 hydrochloride | CP-24879 HCl | Others |
CP-24879 hydrochloride (CP-24879 HCl), a Δ5D/Δ6D dual-inhibitor, can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 hydrochloride exhibits superior antisteatotic an... | |||
T25428 | Flufiprole | Rizazole,Butene-fipronil | |
Flufiprole is used as a phenylpyrazole pesticide. It has enantioselective metabolism in human and rat liver microsomes. | |||
T27567 | IAA-94 | IAA94,IAA 94 | |
IAA-94 is an inhibitor of chloride channels, it binds channels in bovine kidney cortex microsomes with a Ki value of 1 µM. | |||
T37210 | 5-hydroxy Indomethacin | ||
5-hydroxy Indomethacin is a metabolite of indomethacin .1It is formed from indomethacin in rabbit hepatic microsomes. 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fet... | |||
T70091 | IACS-4759 | ||
IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes. | |||
T37229 | (±)8,9-DiHETE | ||
(±)8,9-DiHETE is a major metabolite of the 20:5 ω-3 fatty acid eicosapentaenoic acid .[1] It is produced in rat liver microsomes, but not renal microsomes, by the generation of the unstable intermediate 8,9-epoxy eicosa... | |||
T32912 | Lu49888 HCl | Azidopamil,LU49888,LU 49888,Ludopamil,LU-49888 | |
LU 49888 is a photoaffinity analog of verapamil that has been used to identify specific binding sites for phenylalkylamines of calcium channels present in rabbit skeletal muscle microsomes. | |||
T37306 | 6-hydroxy Chlorzoxazone | 6-hydroxy Chlorzoxazone,NSC 24955 | |
6-hydroxy Chlorzoxazone is a metabolite of chlorzoxazone. [1] It is formed by metabolism of chlorzoxazone by the cytochrome P450 (CYP) isoform CYP2E1 in human hepatic microsomes. | |||
T37430 | Mirtazapine N-oxide | ||
Mirtazapine N-oxide is a metabolite of mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4 in human liver microsomes. | |||
T36666 | Dehydro Warfarin | ||
Dehydro warfarin is a metabolite of (±)-warfarin .1It is formed from (±)-warfarin by rat liver microsomes. 1.Kaminsky, L.S., Fasco, M.J., and Guengerich, F.P.Comparison of different forms of liver, kidney, and lung micro... | |||
T36794 | Dolutegravir O-β-D-Glucuronide | ||
Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized ... | |||
T40238 | Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium | Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium | |
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) displays a prolonged half-life (t1/2) compared to tenofovir in human liver microsomes. Moreover, it demonstrates potent in vitro anti-HIV activity and improves in viv... | |||
T40239 | Tenofovir-C3-O-C15-CF3 ammonium | Tenofovir-C3-O-C15-CF3 ammonium | |
Tenofovir-C3-O-C15-CF3 (ammonium) demonstrates prolonged half-life values compared to tenofovir in human liver microsomes. It exhibits potent anti-HIV activity in vitro and enhances pharmacokinetic properties in vivo. | |||
T35919 | N-hydroxy Riluzole | ||
N-hydroxy Riluzole is a metabolite of the antiglutamatergic agent riluzole .1It is formed from riluzole predominantly by the cytochrome P450 (CYP) isoform CYP1A2 in human hepatic microsomes. 1.Sanderink, G.J., Bournique,... | |||
T35715 | N-desmethyl Eletriptan | ||
N-desmethyl Eletriptan is a metabolite of eletriptan .1It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes. 1.Evans, D.C., O’Connor, D., Lake, B.G., et al.Eletript... | |||
T13658 | DMEA-PNU-159682 | Others | |
DMEA-PNU-159682 (molecule D12) is an ADC cytotoxin molecule, including neomycin (MMDX) metabolites from liver microsomes and effective ADC cytotoxin PNU-159682. | |||
T25826 | MMV024101 | MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101 | |
MMV024101 is a PI4K inhibitor. MMV024101 exhibits submicromolar potency against P. falciparum NF54 (IC50 =543 nM), low aqueous solubility (<5 μM), and rapid clearance by mouse liver microsomes with only 2% of parent comp... | |||
T28156 | Nepaprazole | TY-11345,TY11345,TY 11345 | |
Nepaprazole is a proton pump inhibitor. TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes, and the inhibitory effect was enhanced under weak acid conditions, the IC50 being... | |||
T35997 | 22-HDHA | ||
22-HDHA 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 micr... | |||
T17802 | DBCO-PEG4-VC-PAB-DMEA-PNU-159682 | Others | |
DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), comprises the ADC linker DBCO-PEG4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. The cytotoxin includes metabolites of ... | |||
T35512 | (±)16-HDHA | ||
(±)16-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)16-HDHA is a potential marker of oxidative stre... | |||
T36607 | (±)8-HDHA | ||
(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress... | |||
T64190 | Keap1-Nrf2-IN-12 | ||
eap1-Nrf2-IN-12 is a potent inhibitor of Keap1-Nrf2 (IC50: 2.30 μM). eap1-Nrf2-IN-12 is metabolically stable in human liver microsomes. | |||
T36058 | Dibutyl-3-Hydroxybutyl Phosphate | ||
Dibutyl 3-hydroxybutyl phosphate is a compound produced from the metabolism of the organophosphorus solvent, tributyl phosphate (TBP). Incubation of goldfish liver microsomes in the presence of NADPH has been shown to co... | |||
T18302 | Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 | Others | |
Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate utilized in antibody-drug conjugate (ADC) therapy. It comprises the ADC linker Mal-Phe-C4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 ... | |||
T61136 | Enpp-1-IN-11 | ||
Enpp-1-IN-11 (compound 23) is a highly potent inhibitor of Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1), with a Ki value of 45 nM. It demonstrates excellent stability in human and mouse plasma and exhibit... | |||
T37440 | C2 Adamantanyl Galactosylceramide (d18:1/2:0) | ||
C2 Adamantanyl Galactosylceramide (d18:1/2:0) (AdaGalCer) is a bioactive sphingolipid. It reduces globotriaosylceramide 3 synthesis from exogenous lactosylceramide in microsomes. AdaGalCer stimulates recombinant glucocer... | |||
T73148 | ACT-777991 | ||
ACT-777991 is an orally active, selective CXCR3 antagonist with demonstrated stability in microsomes and hepatocytes across various animal models. This compound effectively inhibits the migration of activated T cells tow... | |||
T36840 | (R)-Omeprazole (sodium salt) | ||
(R)-Omeprazole is the inactive isomer of omeprazole , a gastric proton-pump inhibitor. A stereoselective hydroxylation of (R)-omeprazole is mediated primarily by cytochrome P450 (CYP) 2C19, whereas CYP3A4 favors sulfoxid... | |||
T18292 | Mal-PEG4-VC-PAB-DMEA-PNU-159682 | Others | |
Mal-PEG4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) therapy. It combines the ADC linker, Mal-PEG4-VC-PAB, with the potent ADC cytotoxin, DMEA-PNU-159682. The cytotoxin, D... |
カタログ番号 | 製品名 | 別名 | ターゲット |
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TN3255 | 7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone | Others | |
7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone shows diacylglycerol acyltransferase (DGAT)1 inhibition with IC(50) values of 47.0 microM (for rat liver microsomes) and 160.7 m... | |||
T13618 | Citreoviridin | Others | |
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na+/K+-ATPase whereas, in microsomes, both Na+/K+-ATPase and Mg2+-ATPase activities are significantly stimulated in a dose-depen... | |||
T13679 | Enniatin B | ERK | |
Enniatins B decreases the activation of ERK (p44/p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liv... | |||
T36776 | Terpendole C | ||
Terpendole C is an indole diterpene alkaloid fungal metabolite originally isolated from A. yamanashiensis and an inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 2.1 μM in rat liver microsomes). It ... | |||
T11201 | Enniatin A1 | ERK | |
Enniatin A1, a cyclic hexadepsipeptide composed of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids isolated from Fusarium mycotoxins, exhibits anticarcinogenic effects through the induction of apoptosi... | |||
T83264 | 6-Hydroxy-TSU-68 | ||
6-Hydroxy-TSU-68, a derivative and metabolite of TSU-68, reflects the compound's self-induced hydroxylation in human liver microsomes [1]. | |||
T35400 | β-Muricholic Acid | β-MCA,5β-Cholanic Acid-3α,6β,7β-triol,β-Muricholic Acid | |
β-Muricholic acid (β-MCA) is a murine-specific primary bile acid.[1],[2] Dietary administration of β-MCA reduces HMG-CoA reductase activity in liver microsomes from mice fed a high cholesterol and cholic acid diet.[3] Di... | |||
T37774 | Thielavin A | ||
Thielavin A is a fungal metabolite originally isolated from T. terricola that is related to thielavin B . Thielavin A inhibits COX, blocking both the conversion of arachidonic acid to prostaglandin H2 and the conversion ... | |||
T83241 | 7-Hydroxy-TSU-68 | ||
7-Hydroxy-TSU-68 is a derivative and metabolite of TSU-68, originating from the self-induced hydroxylation of TSU-68 in human liver microsomes, indicative of its biotransformation pathway [1]. | |||
T37690 | Phenylpyropene A | ||
Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).... | |||
T13678 | Enniatin A | ||
Enniatin A, a Fusarium mycotoxin, inhibits acyl-CoA: cholesterol acyltransferase (ACAT) with an IC50 of 22 μM in rat liver microsome enzyme assays. | |||
T13680 | Enniatin B1 | ERK | |
Enniatin B1, a Fusarium mycotoxin, crosses the blood-brain barrier, decreases the activation of ERK (p44/p42), and inhibits moderately TNF-α-induced NF-κB activation. Furthermore, it inhibits acyl-CoA: cholesterol acyltr... |
カタログ番号 | 製品名 | Species | Expression System |
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TMPH-01748 | CYPOR Protein, Human, Recombinant (GST) | Human | E. coli |
This enzyme is required for electron transfer from NADP to cytochrome P450 in microsomes. It can also provide electron transfer to heme oxygenase and cytochrome B5. CYPOR Protein, Human, Recombinant (GST) is expressed in... | |||
TMPY-03414 | ABHD10 Protein, Human, Recombinant (aa 53-306, His) | Human | Baculovirus Insect Cells |
Mycophenolic acid (MPA), the active metabolite of the immunosuppressant mycophenolate mofetil (MMF), is primarily metabolized by glucuronidation to a phenolic glucuronide (MPAG) and an acyl glucuronide (AcMPAG). It is... |