ApNA 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…

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…

A 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.

A 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.

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 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.

CAY10514 is an aromatic analog of 8(S)-HETE. It acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 µM, respectively.

Selective inhibitor of monoacylglycerol hydrolysis; blocks 2-oleoyl glycerol hydrolysis in the cytosolic (IC50 = 4.5 µM) and membrane (IC50 = 19 µM) fractions of rat cerebella.

A potent activator of Nrf2-regulated activity, both in vitro (10 μM) and in mice (50 mg/kg).

Latanoprost is an F-series PG analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as an FP…

An analog of AEA with no intrinsic binding affinity for either CB1 or CB2 receptors; potently inhibits AEA reuptake in U937 lymphoma cells (IC₅₀ = 3 µM); may enhance endocannabinoid signalling by augmenting endocannabinoid concentrations.

An analog of AEA that exhibits weak or no binding to the human CB1 receptor (Ki >1 µM); inhibits rat glial gap junction cell-cell communication at a concentration of 50 µM.

Latanoprost is the isopropyl ester of 17-phenyl-13,14-dihydro PGF2α. It is a prodrug form of the free acid, which is a potent agonist of the FP receptor in the eye. Latanoprost reduces intraocular pressure in glaucoma patients with few side effects. The EC₅₀ value of latanoprost…

A 3-furyl arachidonoyl analog that acts as a potent and selective reuptake inhibitor of AEA (IC50 = 0.8 µM) but has low affinity for FAAH (IC50 = 30 µM); potentiates the biological effects of AEA when co-administered in rats.

A hybrid lipoic acid-TZD derivative that transactivates human PPARγ with an EC50 value of 10 µM.

Latanoprost is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. 5-trans Latanoprost is an isomer of latanoprost wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an…

An inhibitor of FAAH attenuating the FAAH activity from mouse neuroblastoma cells with an IC₅₀ value of 12 µM; alters both the Km and the Vmax of FAAH, indicating that it is a very tight binding, competitive inhibitor; does not inhibit cPLA2 and is essentially devoid of…

A nitroaniline fatty acid amide used to measure FAAH activity; exposure to FAAH activity results in the release of the yellow colorimetric dye m-nitroaniline (ε = 13,500 at 410 nm) allowing the fast and convenient measurement of FAAH activity using a 96-well plate spectrophotometer.

An analog of AEA that binds to the human CB1 receptor with a Ki value of 60 nM; inhibits rat glial gap junction cell-cell communication at a concentration of 50 µM.

A potent, non-selective COX-2 inhibitor (IC₅₀ = 0.04 µM); >1,700 times more potent as an inhibitor of COX-2 than COX-1.

An arachidonoyl amino acid isolated from both rat and bovine brain; the glycine congener (NAGly; Item No. 90051) suppresses formalin-induced pain in rats, but NAG-3H-ABA has not yet been fully characterized.

Unoprostone is an analog of PGF2α with a 13,14-dihydro-15-keto modification and a two-carbon extension of the aliphatic lower side chain. The isopropyl ester of unoprostone (Catalog No. 16681) (Rescula) has been approved for clinical use as an ocular hypotensive drug.

Arachidonamide is an analog of AEA that lacks the hydroxyethyl moiety. It is hydrolyzed by FAAH more effectively than AEA but exhibits significantly weaker binding to the human CB1 receptor with a Ki value of 9.6 µM. Arachidonamide and AEA exhibit similar binding and translocation into cells…

A potent, stable, and selective agonist analog of AEA with a Ki value of 1.4 nM at the isolated rat CB1 receptor; 1,400 times more potent at the CB1 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 receptor…

Misoprostol is a prostaglandin E1 (Item No. 13010) analog with agonist activity mediated by EP2, EP3, and EP4 receptors. It has been shown to inhibit the formation of gastric lesions in rats (ED₅₀ = 0.31 µg/kg),{1754} inhibit superoxide generation in human neutrophils…