Biologically Active Small Molecules, 5 mg, UN1170
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N-Arachidonyl Maleimide
Cayman ChemicalNAM is a potent, irreversible inhibitor of MAGL or MAGL-like activity in rat cerebellar membranes, exhibiting an IC50 value of 140 nM. Inhibition of MAGL by the sulfhydryl-reactive maleimide group of NAM suggests a critical cysteine residue is present in the substrate-binding site of the enzyme.
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5-Iodotubercidin
Cayman ChemicalInitiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).
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ß-Nicotyrine
Cayman ChemicalAn alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.
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HEPC
Cayman ChemicalThioester analogs of glycerophospholipids, in combination with Ellman’s reagent, are convenient colorimetric substrates for the measurement of phospholipase activity. HEPC is a truncated analog of phosphatidylcholine with the entire sn-1 substituent deleted, and with a hexadecylthioester in…
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5-trans Fluprostenol isopropyl ester
Cayman ChemicalTravoprost is the Alcon trade name for fluprostenol isopropyl ester, an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. Fluprostenol isopropyl ester is a prodrug which is converted by esterase enzymatic activity in the cornea to yield the corresponding…
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Docosahexaenoyl Ethanolamide
Cayman ChemicalThe ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…
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Thioetheramide-PC
Cayman ChemicalThioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of sPLA2. The IC50 value for thioetheramide-PC is 2 µM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, thioetheramide-PC…
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cis-4,10,13,16-Docosatetraenoic Acid methyl ester
Cayman Chemicalcis-4,10-13,16-Docosatetraenoic acid methyl ester is a long chain PUFA. It is a minor fatty acid component of rat testis lipids. The methyl ester is a neutral, more lipophilic form of the free acid.
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L-902,688
Cayman ChemicalA potent and selective agonist of the human PGE2 receptor, EP4 with a Ki value of 0.38 nM and an EC50 value of 0.6 nM; induces thermal hyperalgesia when injected into guinea pig forepaw and increases vasodilation of human pulmonary vein.
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4-hydroxy Nonenal
Cayman ChemicalA lipid peroxidation product derived from oxidized ω-6 PUFAs such as linoleic acid and arachidonic acid which is widely used as a marker of lipid peroxidation.
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?-Tocotrienol
Cayman ChemicalSpontaneously hypertensive rats fed a diet which includes γ-tocotrienol show significant reduction of systolic blood pressure and an increase of nitric oxide synthase activity in blood vessels. γ-Tocotrienol at 20 µM induces apoptosis of malignant sympathoadrenal (+SA) murine…
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AM404
Cayman ChemicalAn analog of AEA that potentiates the activity of endogenous AEA by blocking its re-uptake into presynaptic neurons; selectively inhibits the carrier-mediated transport of AEA without affecting anandamide hydrolysis; inhibits the transport of AEA with an IC50 value of 1 µM in rat…
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(R)-(-)-Docosahexaenyl-2'-Hydroxy-1'-Propylamide
Cayman ChemicalA homolog of DHEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.
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CAY10580
Cayman ChemicalAn 8-aza-9-oxo-15-hydroxy saturated analog of PGE2; selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3,000, 2,000, and >3,000 nM, respectively); stimulates cAMP formation in excised mouse ovaries.
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Eicosapentaenoyl Ethanolamide
Cayman ChemicalAn N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.
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(R,S)-Anatabine
Cayman ChemicalA minor alkaloid produced in plants of the Solanaceae family, including tobacco; detection in urine is used as an indicator of tobacco use; diminishes Aβ production, reduces the transcription and protein levels of β-secretase, and dose dependently inhibits NF-κB activation.
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PAF C-18:1
Cayman ChemicalA naturally occurring phospholipid produced by cells upon inflammatory stimulation; less potent than PAF C-16 and PAF C-18 in the induction of neutrophil chemotaxis, but is equipotent to PAF C-16 and PAF C-18 in promoting eosinophil migration.
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Oleoyl Serotonin-d17
Cayman ChemicalAn internal standard for the quantification of oleoyl serotonin by GC- or LC-MS.
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PPHP
Cayman ChemicalPPHP is a substrate for the measurement of peroxidase enzymes. PPHP has been used to quantitate the peroxidase activity of COX-1 and COX-2.
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Eicosapentaenoyl 1-propanol-2-amide
Cayman ChemicalAn EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 µM; an analog of EPEA, a natural N-acylethanolamide that impacts aging and inflammation.
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Argatroban
Cayman ChemicalA reversible, competitive thrombin inhibitor (Ki = 5 nM) that shows selectivity for thrombin over other clotting pathway enzymes.
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8-iso Misoprostol
Cayman Chemical8-iso Misoprostol is one of several possible impurities in the production of bulk commercial preparations of misoprostol, and one that is somewhat difficult to distinguish from other impurities such as 11β-misoprostol. The pharmacology and EP receptor binding affinity for 8-iso misoprostol has…
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Oleoyl Ethanolamide-d4
Cayman ChemicalAn internal standard for the quantification of OEA by GC- or LC-MS.
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Ionomycin
Cayman ChemicalA selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.
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(S)-a-Methylbenzyl Ricinoleamide
Cayman ChemicalA fatty acid amide derived from ricinoleic acid and methyl benzylamine that demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 µM.
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Arachidonoyl Cyclopropylamide
Cayman ChemicalA potent, stable, and selective agonist analog of AEA with a Ki value of 2.2 nM at the isolated rat CB1 receptor; 325 times more potent at the CB1 receptor compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1…
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(+)-5-trans Cloprostenol
Cayman ChemicalA minor impurity produced in the synthesis of (+)-cloprostenol; 20-fold less active than (+)-cloprostenol in terminating pregnancy in the hamster.
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(R)-(-)-Eicosapentaenyl-2'-Hydroxy-1'-Propylamide
Cayman ChemicalA homolog of EPEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.
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Hydroxy Linoleins
Cayman ChemicalHydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…
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N-(3-hydroxyphenyl)-Arachidonoyl amide
Cayman Chemical3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.