Biologically Active Small Molecules, UN1231

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UN1231 Biologically Active Small Molecules

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  • 17-phenyl trinor PGA2 is a synthetic prostaglandin analog designed for increased half-life and greater potency. There are no published reports of the biological activity of 17-phenyl trinor PGA2 in the literature at this time.

  • Cayman Chemical

    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…

  • 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…

  • Cayman Chemical

    Misoprostol is a widely sold analog of PGE1 which has potent but relatively non-selective agonist activity with respect to the prostanoid EP receptor subgroup. Misoprostol has been used therapeutically for many years in humans for the treatment of gastric ulcer disease under the Searle tradename…

  • Cayman Chemical

    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.

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

  • A major urinary metabolite of PGE2 that is excreted in guinea pig urine at a concentration range of 1.34-2.74.

  • Active metabolite of lactacystin, a widely used selective inhibitor of the 20S proteasome, with at least 10 times better activity; irreversibly alkylates subunit X of the 20S proteasome.

  • 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.

  • Cayman Chemical

    A dehydration product of PGD2 formed by the elimination of the C-9 hydroxyl group; inhibits platelet aggregation (IC50 ~ 5-10 nM); has antimitotic and antiproliferative effects on a variety of cultured normal cells and tumor cell lines.

  • Cayman Chemical

    8-iso PGF2β is an isomer of PGF2α with a non-enzymatic, non-cyclooxygenase origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and…

  • 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 8-iso PGF2β via the 15-hydroxy PGDH pathway.

  • Cayman Chemical

    Unoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…

  • 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.

  • Cayman Chemical

    A dehydration product of tetranor-PGEM that can be measured as a surrogate for tetranor-PGEM levels in urine.

  • Cayman Chemical

    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.

  • Cayman Chemical

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

  • PGF2α-NEt is an analog of PGF2α in which the C-1 carboxyl group has been modified to an N-ethyl amide. PG esters have been shown to have ocular hypotensive activity. PG N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been…

  • Cayman Chemical

    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).

  • ACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…

  • An internal standard for quantification of 13,14-dihydro-15 (R,S)-hydroxy-16,16-difluoro-Prostaglandin E1, a metabolite of a bicyclic PGE1 derivative used in the treatment of chronic constipation, by GC- or LC-mass spectrometry (MS).

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

  • Cayman Chemical

    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.

  • Cayman Chemical

    Butaprost is a structural analog of PGE2 with good selectivity for the EP2 receptor subtype. Butaprost has frequently been used to pharmacologically define the EP receptor expression profile of various human and animal tissues and cells. Serious confusion as to the structure of Butaprost was…

  • Cayman Chemical

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

  • 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.

  • Cayman Chemical

    A FAHFA consisting of palmitoleic acid esterified at the 9-position of hydroxy stearic acid; significantly elevated in serum of glucose tolerant AG4OX mice; may be a bioactive lipid with roles in metabolic syndrome and inflammation.

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

  • Cayman Chemical

    A form of FAHFA in which oleic acid is esterified to 13-hydroxy stearic acid.

  • Cayman Chemical

    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…

  • Cayman Chemical

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

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