A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

Cloprostenol is a synthetic PGF2α analog and a potent FP receptor agonist. (+)-15-epi Cloprostenol is the 15(S), or 15β-hydroxy enantiomer of (+)-cloprostenol. This epimer is less active by several orders of magnitude as an FP receptor ligand when compared to 15(R)-cloprostenol. However,…

An angiotensin metabolite that functions as a type 1 angiotensin II receptor agonist whereupon it can control hydroelectrolyte balance and demonstrates vasodilatory and anti-inflammatory actions in opposition to various adverse effects of angiotensin II.

Functions as a potent laxative by inducing chloride secretion in colonic mucosa and releasing acetylcholine, which stimulates contraction of intestinal smooth muscle; also demonstrates anti-tumor activity (ED50s = 1-13 µM), inducing apoptosis in various cancer cells.

One of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid.

A major inactive metabolite of clopidogrel that is used as a reference standard for quantitative analysis of clopidogrel metabolism.

A skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions.

A nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.

The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1 and CRTH2/DP2. 15(R)-15-methyl PGD2 is a potent,…

A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC₅₀ = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

A bioactive sterol that can affect cholesterol homeostasis, membrane properties and cell survival; inhibits CYP7A1 with an IC₅₀ = ~ 1 µM; can be used as a standard in the determination of cholesterol derivatives by GC-MS or HPLC.

The reduced form of the electron acceptor NADP+ and acts as an electron donor in various biological reactions.

A polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM); acts as a non-specific competitor of…

A steroid hormone produced in the cortex of the adrenal glands that binds to both glucocorticoid and mineralocorticoid receptors; also is the precursor to aldosterone synthesis.

Primary plasma metabolite of PGD2; levels increase nearly 3-fold upon allergan-induced bronchoconstriction in asthmatics.

A small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

A potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.

An orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.

A calcimimetic compound that can allosterically activate or positively modulate the human CaSR; dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials.

An irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases; at 20-200 µM arrests human epidermoid carcinoma A431 cells at mitotic metaphase; inhibits protease-resistant protein accumulation in scrapie-infected neuroblastoma cells (IC₅₀ = 0.5 µM).

A catatoxic steroid that acts as an agonist of the rodent PXR at µM concentrations; mediates induction of hepatic CYP3A, Oatp2, and Cyp7a1, regulating both xenobiotic and bile acid homeostasis.

A small molecule pan activator of Ras-related GTPases, activating Rac1, cdc42, Ras, and Rab-2A with EC₅₀ values of 20, 100, 141, and 355 nM, respectively.

A thymidine analog that is readily incorporated, following phosphorylation, into newly synthesized DNA in place of thymidine; can be detected immunologically in cells and tissues.

A reversible and competitive inhibitor of type IV collagen-specific MMP-2 and MMP-9 with preference towards MMP-2 (IC50 = 4 and 20 µM, respectively).

A potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

A selective SGLT2 inhibitor (IC₅₀ = 3.1 nM) that has been shown in clinical trials of patients with type 2 diabetes to lower fasting and postprandial glucose levels by increasing total glucose excretion, improving β-cell function, and shifting substrate utilization from glucose to lipids.

A monohydroperoxy PUFA produced by the action of 15-LO on γ-linolenic acid.

A potent, orally bioavailable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki death proteins, like Bim, leading to apoptosis; induces apoptosis in cancer cell lines expressing mutants of β-catenin 1.

L-Carnitine is an endogenous quaternary ammonium compound required for fatty acid transport; it is often given as a dietary supplement. The L-isomer is active, exhibiting anti-osteoporotic, antioxidative, and cardioprotective activities. In a clinical setting, L-carnitine administration increases…

An irreversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase (CSE) (IC50 value of 55 µM).

An intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.

Allicin is an thiocyanate found in garlic; it exhibits a wide variety of properties, including anticancer, antioxidative, antihypertensive, anti-arrhythmic, anti-parasitic, and anti-diabetic activities. In vitro, allicin binds cellular nucleic acid, primarily nitrogenous bases and phosphate…