A methyl ester prodrug form of the NOS inhibitor L-NNA; exhibits Ki values of 15 nM, 39 nM, and 4.4 µM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively.

Diethylstilbestrol (DES) is a synthetic estrogen receptor agonist that was prescribed to pregnant women in the late 1930s. It was banned in 1971 because of possible links to increased risk of breast cancer in mothers along with congenital abnormalities and increased risk of cancer in offspring. DES…

A time-dependent, non-specific COX inhibitor with IC₅₀ values of 1.5 and 9.7 µM for human recombinant COX-1 and COX-2, respectively.

An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, and other legumes; acts as a tyrosine kinase inhibitor, has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors.

A synthetic glucocorticoid that binds the human glucocorticoid receptor with a higher affinity than a natural ligand, cortisol (Kd = 5 vs. 17 nM, respectively); has anti-inflammatory effects.

A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

A non-selective COX inhibitor with IC₅₀ values for ovine COX-1 and -2 of 0.1 and 6 µM, respectively; IC₅₀ values for human recombinant COX-1 and -2 are 1.67 and 24.6 µM, respectively.

Bezafibrate is a well established pan-PPAR activator. This fibrate drug has over 25 years of therapeutic use with a good safety profile. The fibrate class of drugs are generally known as PPARα agonists, but bezafibrate appears to activate PPAR.delta. and PPARγ as well. Bezafibrate…

A progestin that is a racemic mixture of which levonorgestrel is the biologically active component.

Saturated fatty acids are synthesized by both plants and animals from acetyl coenzyme A as a form of long-term energy storage. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of the normal human dietary fat intake, and approximately 25% of the total plasma fatty acids in…

Estrone is one of the three naturally occurring estrogens, the others being estradiol and estriol. Estrone is synthesized from androstenedione by the aromatase enzyme system in the ovaries and placenta, and is also synthesized from estradiol by 17-hydroxy steroid dehydrogenase in the liver. Serum…

(S)-Naproxen is a non-selective COX inhibitor. The IC₅₀ values for human recombinant COX-1 and -2 are 0.6-4.8 µM and 2.0-28.4 µM, respectively.

Chlorogenic acid is a phenolic natural product isolated from the leaves and fruits of dicotyledonous plants, including the coffee bean. Structurally, chlorogenic acid is the ester of caffeic acid with the 3-hydroxyl group of quinic acid. Chlorogenic acid is an important factor in plant metabolism.…

A potent PR and GR antagonist with Ki value of approximately 1 nM.

The major estrogen secreted by the premenopausal ovary.

The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

A synthetic intermediate useful for pharmaceutical synthesis.

Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in…

A long-chain saturated fatty acid that does not affect plasma total cholesterol or LDL-cholesterol but may reduce HDL-cholesterol.

Linoleic acid is an essential fatty acid and one of the most abundant PUFAs in the western diet. Deficiencies in linoleic acid are linked to defective wound healing, growth retardation, and dermatitis. Linoleic acid is metabolized by 15-LO in both plants and animals to form 9- and 13-HODE.

A major flavonolignan from the extracts of milk thistle seed, S. marianum; blocks the production of superoxide in PMA-activated rat Kupffer cells (EC50 = ~100 µM); inhibits the synthesis of LTB4 (IC50 = ~15 µM).

A PPARα agonist and hypolipidemic drug used clinically to treat dyslipidemia and cardiovascular disease; exhibits EC50 values of 18 and 30 µM for mouse and human PPARα, respectively.

An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, clover, kudzu, and other legumes.

Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the treatment of osteoporosis.{12450} Three major metabolites of tibolone are responsible for its tissue selective mechanism of action.…

Phenylbutazone is a NSAID and efficient reducing cofactor for the peroxidase activity of COX. It enhances hydrogen peroxide inactivation of both COX and PGI synthase.

A synthetic intermediate or building block for drug discovery or pharmaceutical synthesis.

Hydroxymethyl uracil is a product of oxidative damage to DNA, predominantly by hydroxyl radical via the Fenton reaction.

An alkaloid natural product that reduces total cholesterol, LDL cholesterol, and triglycerides in humans and hamsters; enhances LDL-receptor protein and mRNA levels in hepatocytes.

Ricinoleic acid methyl ester is a neutral, more lipophilic form of the free acid that can be used as an analytical standard for ricinoleic acid.

A synthetic intermediate useful for pharmaceutical synthesis.

A synthetic intermediate useful for pharmaceutical synthesis.