Biologically Active Small Molecules, Cayman Chemical, UN1231
-
Tafluprost ethyl amide
Cayman ChemicalA more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).
-
13,14-dihydro-15(R,S)-hydroxy-16,16-difluoro Prostaglandin E1-d4
Cayman ChemicalAn 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).
-
-
11ß-Misoprostol
Cayman ChemicalMisoprostol 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…
-
11ß-Prostaglandin E2
Cayman Chemical11β-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…
-
8-iso-15-keto Prostaglandin F2ß
Cayman ChemicalA potential metabolite of 8-iso PGF2β via the 15-hydroxy PGDH pathway.
-
ent-Prostaglandin E2
Cayman ChemicalEnzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings…
-
Oleic Acid-2,6-diisopropylanilide
Cayman ChemicalACAT 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…
-
Prostaglandin J2
Cayman ChemicalA 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.
-
17-phenyl trinor Prostaglandin A2
Cayman Chemical17-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.
-
Methyl a-Linolenyl Fluorophosphonate
Cayman ChemicalAn analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the α-linolenyl analog of MAFP has not been completely investigated.
-
15-deoxy-?12,14-Prostaglandin A1
Cayman ChemicalA synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.
-
20-ethyl Prostaglandin E2
Cayman Chemical20-ethyl PGE2 is an analog of PGE2 in which the ω-chain has been extended by the addition of two methylene carbon atoms. The only well studied prostaglandin analog with this structural feature is unoprostone, an F-series prostaglandin that is clinically approved as a glaucoma medication.…
-
Iloprost
Cayman ChemicalIloprost 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…
-
Arachidonoyl p-Nitroaniline
Cayman ChemicalApNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate AEA (Item No. 90050). It also will hydrolyze…
-
17-trans Prostaglandin E3
Cayman Chemical17-trans PGE3 is an isomer of PGE3 which could theoretically result from the COX metabolism of dietary trans-fatty acids. There are no published reports on the biological activity of this compound.
-
8-iso Prostaglandin A1
Cayman Chemical8-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.
-
13,14-dihydro-15-keto Prostaglandin F1a
Cayman Chemical13,14-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.
-
Unoprostone isopropyl ester
Cayman ChemicalUnoprostone 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…
-
tetranor-PGAM
Cayman ChemicalA dehydration product of tetranor-PGEM that can be measured as a surrogate for tetranor-PGEM levels in urine.
-
8-iso-17-phenyl trinor Prostaglandin F2ß
Cayman Chemical8-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.
-
15(S)-Latanoprost
Cayman ChemicalAn 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.
-
N-acetyl-S-farnesyl-L-Cysteine
Cayman ChemicalAFC 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.
-
-
13,14-dihydro-15-keto Prostaglandin F2a
Cayman ChemicalProminent plasma metabolite of PGF2α in the 15-hydroxy PGDH pathway.
-
Octyl-a-ketoglutarate
Cayman ChemicalA 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.
-
(R)-Butaprost
Cayman ChemicalButaprost 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…
-
15(R)-17-phenyl trinor Prostaglandin F2a isopropyl ester
Cayman ChemicalA latanoprost-related isomer containing both a double bond at C-13,14 and an invered (b) hydroxyl group at C-15; a potential impurity in most commercial preparations of the lantanoprost bulk drug product.
-
16,16-dimethyl Prostaglandin E2
Cayman ChemicalA 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 Prostaglandin F2ß
Cayman Chemical16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.
-
-
13,14-dihydro-15-keto Prostaglandin E2
Cayman ChemicalThe primary metabolite of PGE2 in plasma which is formed through the 15-hydroxy PGDH pathway.