Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM. Iloprost…

A stable, cell-permeable form of α-ketoglutarate which accumulates rapidly and preferentially in cells with a dysfunctional TCA cycle; stimulates PHD activity and increases HIF-1α turnover when used at 1 mM; competitively blocks succinate- or fumarate-mediated inhibition of PHD.

PGD2 is one of the five primary enzymatic prostaglandins derived directly from PGH2. PGD2 is produced abundantly in the CSF by the lipocalin-type PGD synthase, and in the periphery by myeloid cells including mast cells and basophils by a second, hematopoietic-type PGD synthase. PGD2 is chemically…

13,14-dihydro-15-keto PGF1α is a metabolite of PGF1α that has been reported in the rat stomach. The measurement of 13,14-dihydro-15-keto PGF1α can be used as a marker of the in vivo production of PGF1α.

A lipid peroxidation product; actively modifies histidine and lysine residues on proteins and causes protein cross-linking.

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…

An F-series PG analog in which the C-1 carboxyl group has been modified to an N-diethyl amide; dialkyl amides such as a 17-p-PGF2α-NEt2 are inert to corneal amidase activity, and are not converted in any detectable amount to the corresponding free acids.

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

Prominent plasma metabolite of PGF2α in the 15-hydroxy PGDH pathway.

PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity. At a 25 µM concentration, PGA2 blocks the cell…

TXA2 receptor agonist; causes platelet shape change (EC₅₀ ~6 nM) and aggregation (EC₅₀ ~97 nM).

PGB2 is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 µg/kg).

8-iso PGA1 is an isoprostane and a member in a large family of prostanoids of non-cyclooxygenase origin. It occurs as a common minor impurity in most commercial preparations of PGE1. The biological activity of 8-iso PGA1 has not been studied in depth or reported in the literature.

A potent and selective G9a HMTase inhibitor (IC50 = 6 nM; Ki = 63 pM); more than 40,000-fold selective for G9a over SET7/9, SET8, PRMT3, and JMJD2E.

Contains four deuterium atoms at the 3', 3', 4', and 4' positions; is intended for use as an internal standard for the quantification of tafluprost by GC-or LC-mass spectrometry.

8-iso-17-phenyl PGF2β is an isomer of bimatoprost (free acid) that is epimerized at the 8 and 9 positions. There are no published reports on the biological activity of 8-iso-17-phenyl PGF2β.

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 9β-hydroxy isomer of 5-trans PGF2α.

An analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC₅₀ value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.

An isomer of 17-phenyl trinor PGF2α, characterized by an inverted (β) hydroxyl group at C-15.

An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.

A competitive inhibitor of 15-hydroxy PGDH; acts as an agonist on most EP receptor subtypes (Kd d~ 1 nM for isolated EP2 receptors); preserves the self-renewal properties while preventing the differentiation of hematopoietic stem cells during expansion in culture.

16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.

A potential metabolite of bimatoprost when administered to animals; potential minor impurity in commercial preparations of bimatoprost.

A synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.

A metabolite of PGD2 via the 15-hydroxy PGDH pathway.

15(S)-15-methyl PGF2α is a metabolically stable analog of PGF2α. It is a potent uterine stimulant and abortifacient which can be administered intramuscularly to induce labor. It induces luteolysis and reduces serum progesterone concentrations when given as an intramuscular injection in…

A FAHFA in which oleic acid occurs at the 12-position on hydroxy stearic acid.

An internal standard for the quantification of CAY10429 by GC- or LC-MS.

Bicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…

An internal standard for the quantification of PGA2 by GC- or LC-MS.

An internal standard for the quantification of linoleic acid by GC- or LC-MS.