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Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor
Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM. -
PPARδ agonist
Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1. -
biomarker
N6-Etheno 2'-deoxyadenosine is a reactive oxygen species (ROS)/reactive nitrogen species (RNS)-induced DNA oxidation product, used as a biomarker to evaluate chronic inflammation and lipid peroxidation in animal or human tissues. -
MAO-B inhibitor
Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. -
PDE3 inhibitor
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux. - Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
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15-LO inhibitor
PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis. -
MAO Inhibitor
Bifemelane hydrochloride is an antidepressant MAO inhibitor. Reverses catalepsy induced by tetrabenazine in mice and increases locomotor activity in MPTP-treated marmosets. -
LSD1/BHC110 & MAO inhibitor
Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor. -
Fluorescent P450 substrate
3-Cyano-7-ethoxycoumarin is a fluorogenic substrate suitable for the continuous determination of cytochrome P450 mixed-function monooxygenases. It is a fluorescent probe useful in microsomal dealkylase studies. -
cytochrome P450 substrate
Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes. -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
HMG-CoA Reductase inhibitor
Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.
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PDE10A inhibitor
PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.
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CETP inhibitor
JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis. -
CETP inhibitor
Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM. -
Cathepsin K Inhibitor
Odanacatib is an inhibitor of cathepsin K,an enzyme involved in bone resorption. -
Hsp90 inhibitor
IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90). -
CYP3A Inhibitor
Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate. - Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.
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ACE inhibitor/Beta blocker
Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. -
PDE-2 Inhibitor
BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). - Calcifediol is a major circulating metabolite of vitamin D3 and acts as a competitive inhibitor with an apparent Ki of 3.9 μM. It also suppresses PTH secretion and mRNA (ED50=2 nM)
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Collagen proline hydroxylase inhibitor
Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor. -
SGK1 inhibitor
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
SGK1 inhibitor
EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. - Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.
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Cathepsin Inhibitor
Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. - Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.
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Vitamin D Analog
Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays. -
DHFR inhibitor
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. -
DGAT1 Inhibitor
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

