Biologically Active Small Molecules, UN1231, 1.0 mg, Cayman Chemical
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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…
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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.
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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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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.
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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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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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17-phenyl trinor Prostaglandin F2a diethyl amide
Cayman ChemicalAn 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.
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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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13,14-dihydro-15-keto Prostaglandin F2a
Cayman ChemicalProminent plasma metabolite of PGF2α in the 15-hydroxy PGDH pathway.
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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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U-46619
Cayman ChemicalTXA2 receptor agonist; causes platelet shape change (EC50 ~6 nM) and aggregation (EC50 ~97 nM).
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Prostaglandin B2
Cayman ChemicalPGB2 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).
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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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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.
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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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Methyl y-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 γ-linolenyl analog of MAFP has not been completely investigated.
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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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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.
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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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12-OAHSA
Cayman ChemicalA FAHFA in which oleic acid occurs at the 12-position on hydroxy stearic acid.
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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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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.
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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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15(R)-Prostaglandin F2a
Cayman Chemical15(R)-PGF2α is the C-15 epimer of the naturally occurring mammalian autacoid PGF2α. It has only 25% of the potency of PGF2α in hamster antifertility studies, which may be due to reduced affinity for FP receptors. Compared to PGF2α, 15(R)-PGF2α has a binding affinity of…
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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-OAHSA
Cayman ChemicalA form of FAHFA in which oleic acid is esterified to 13-hydroxy stearic acid.
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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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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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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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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…