Biologically Active Small Molecules, 5 mg, UN1231
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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…
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8-iso Prostaglandin F2ß
Cayman Chemical8-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…
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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.
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13-OAHSA
Cayman ChemicalA form of FAHFA in which oleic acid is esterified to 13-hydroxy stearic acid.
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12-OAHSA
Cayman ChemicalA FAHFA in which oleic acid occurs at the 12-position on hydroxy stearic acid.
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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.
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4-oxo-2-Nonenal
Cayman ChemicalA lipid peroxidation product; actively modifies histidine and lysine residues on proteins and causes protein cross-linking.
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Prostaglandin F2a 1,11-lactone
Cayman ChemicalPGF2α 1,11-lactone is a lipid-soluble internal ester of PGF2α. Hydrolysis of the lactone by plasma esterases readily produces free PGF2α in rats and monkeys, but not in humans. PGF2α 1,11-lactone is active as an antifertility agent with greatly reduced vasoactivity compared…
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U-46619
Cayman ChemicalTXA2 receptor agonist; causes platelet shape change (EC50 ~6 nM) and aggregation (EC50 ~97 nM).
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Tafluprost ethyl amide
Cayman ChemicalA more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).
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13,14-dihydro-15-keto Prostaglandin E2
Cayman ChemicalThe primary metabolite of PGE2 in plasma which is formed through the 15-hydroxy PGDH pathway.
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15(R)-17-phenyl trinor Prostaglandin F2a
Cayman ChemicalAn isomer of 17-phenyl trinor PGF2α, characterized by an inverted (β) hydroxyl group at C-15.
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Bicyclo Prostaglandin E2
Cayman ChemicalBicyclo 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…
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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.…
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Prostaglandin F2a ethyl amide
Cayman ChemicalPGF2α-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…
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9-POHSA
Cayman ChemicalA 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.
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Prostaglandin A2
Cayman ChemicalPGA2 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…
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(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…
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13,14-dihydro-15-keto Prostaglandin F2a
Cayman ChemicalProminent plasma metabolite of PGF2α in the 15-hydroxy PGDH pathway.
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CAY10429-d3
Cayman ChemicalAn internal standard for the quantification of CAY10429 by GC- or LC-MS.
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17-trifluoromethylphenyl-13,14-dihydro trinor Prostaglandin F2a
Cayman ChemicalA number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma. Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.…
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GW 848687X
Cayman ChemicalA potent and selective EP1 receptor antagonist (IC50 = 2.5 nM), with >400-fold selectivity relative to EP2, EP3, EP4, DP1, and IP; has 30-fold selectivity over TP; shows complete anti-hyperalgesic activity in a rat model of chronic inflammatory joint pain.
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?12-Prostaglandin D2
Cayman ChemicalPGD2 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…
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ONO-8711
Cayman ChemicalA potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO3- secretion in the stomach.
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15-keto-17-phenyl trinor Prostaglandin F2a
Cayman ChemicalA potential metabolite of bimatoprost when administered to animals; potential minor impurity in commercial preparations of bimatoprost.
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UNC0321 (trifluoroacetate salt)
Cayman ChemicalA 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.
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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…
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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.
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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.
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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.