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Metabolic Enzyme/Protease

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Cat. No. Product Name Field of Application Chemical Structure
DC28844 Ezetimibe phenoxy glucuronide
Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor.
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DC28843 Hydroxy desmethyl Bosentan
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.
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DC28842 Desmethyl Levofloxacin
Desmethyl Levofloxacin is a metabolite of Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
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DC28841 ent-Ezetimibe
ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
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DC28840 4-Desmethyl Istradefylline
4-Desmethyl Istradefylline is a metabolite of Istradefylline. 4-Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
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DC28839 5β-​Dutasteride
5β-Dutasteride is the S configuration of Dutasteride. 5β-Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
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DC28838 Dihydro Dutasteride
Dihydro Dutasteride is a metabolite of Dutasteride. Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
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DC28837 tert-Buthyl Pitavastatin
tert-Buthyl Pitavastatin is the  metabolite of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
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DC28824 Descarbamoyl cefuroxime
Descarbamoyl cefuroxime is a degradation product of Cefuroxime. Descarbamoyl cefuroxime is also an intermediate for the synthesis of Cephalosporin antibiotics.
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DC28818 (Rac)-5-Keto Fluvastatin
(Rac)-5-Keto Fluvastatin (3-Hydroxy-5-Keto Fluvastatin) is an impurity of Fluvastatin (XU 62320). Fluvastatin is a HMG-CoA reductase inhibitor with an IC50 of 8 nM.
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DC28812 3'-Hydroxy Repaglinide
3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide. Repaglinide is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes.
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DC28794 DHODH-IN-1
DHODH-IN-1 (compound 18d) is a potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 25 nM. DHODH-IN-1 is an inhibitor of pyrimidine biosynthesis pathway.
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DC28793 CYP11B2-IN-1
CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM.
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DC28763 4-Desmethoxy Omeprazole
4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.
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DC28762 Autotaxin-IN-5
Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis.
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DC28761 Autotaxin-IN-4
Autotaxin-IN-4 (compound 51), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat idiopathic pulmonary fibrosis.
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DC28759 Autotaxin-IN-3
Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with an IC50 of 2.4 nM, compound 33, sourced from patent WO2018212534A1.
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DC28753 Lp-PLA2-IN-3
Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
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DC28752 Lp-PLA2-IN-2
Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.
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DC28751 DJ001
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration.
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DC28746 JNJ-42226314
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.
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DC28744 AR453588 hydrochloride
AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.
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DC28743 AR453588
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
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DC28724 5-ALA benzyl ester hydrochloride
5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) is a protoporphyrin precursor used as a photodetection agent. 5-ALA benzyl ester hydrochloride induces protoporphyrin IX (PPIX) accumulation in colon carcinoma cell lines.
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DC28708 ATX inhibitor 5
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 has anti-hepatofibrosis effect, and reduces CCl4-induced hepatic fibrosis level prominently.
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DC28694 5-Hydroxy-2'-deoxyuridine
5-Hydroxy-2'-deoxyuridine (5-OHdU) is a major stable oxidation product of 2'-Deoxycytidine. 5-Hydroxy-2'-deoxyuridine can be incorporated into DNA in vitro by DNA polymerase.
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DC28673 IDO1-IN-2
IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity.
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DC28672 Nampt-IN-5
Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
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DC28607 MJ33 lithium
MJ33 lithium is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 lithium blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6. MJ33 lithium has a critical effect on inflammatory brain damage.
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DC28599 N1,N8-Diacetylspermidine hydrochloride
N1,N8-Diacetylspermidine hydrochloride is a polyamines in the human urine. N1,N8-Diacetylspermidine hydrochloride is useful as prognostic indicators after treatment and during follow-up examination of cancer patients.
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