Metabolism

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.

WAY-362450 is a highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%).

SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor with anticancer properties currently in clinical trials. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent

PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.

KW-2478 is an agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

A 922500 is a diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively).

GW3965 HCl is a selective and orally active liver X receptor (LXR) full agonist.

JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis.

PF 429242 is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease.

Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM.

XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).

IPI-493 is a potent and orally bioavailable HSP90 inhibitor with Ki of 21 nM.

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.

Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis.

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.

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.

BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human).

Calcipotriol is a low-calcemic vitamin D receptor (VDR) agonist.

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)

Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor.

T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.

D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.

Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.

EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.

EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.

Ganetespib is a potent, synthetic, small molecule inhibitor of Hsp90, a chaperone protein that is essential to the function of certain other proteins that drive the growth, proliferation, and survival of many different types of cancer.

MK-8245 is a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor. MK-8245 is useful for the Treatment of Diabetes and Dyslipidemia.

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.

GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.

LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.

Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.

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.

Otamixaban(FXV 673) is an intravenous direct factor Xa inhibitor.

Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

PF-8380 is a potent and specific autotaxin inhibitor with an IC50 value of 2.8 nM.

PDE-9 inhibitor is useful for neurodegenerative diseases.

Paricalcitol is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.

Pentostatin is an irreversible inhibitor of adenosine deaminase (Ki = 2.5 pM).

SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.

SMND-309 is a metabolite of salvianolic acid B, and exhibits neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats.

T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2.

Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.

Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.

Geniposidic acid is an effective anticancer and radioprotection agent.

Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.

Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.

Tioxolone is an anti-acne preparation.