8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a metabolite of the isoprostane 8-iso PGF2α in rabbits, monkeys, and humans. 8-isoprostane (8-iso PGF2α) is a prostaglandin-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-iso PGF2α is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-iso PGF2α is infused into rabbits. Early in the infusion (within 1-2 minutes) 8-iso -15-keto PGF2α was a major component of the metabolite profile, which was comprised mostly of unmetabolized 8-iso PGF2α. 8-iso -15-keto PGF2α is a vasoconstrictor when tested on the rat isolated thoracic aorta, acting via the TP (thromboxane) receptor.
Isoprostanes are produced by the non-enzymatic, free radical peroxidation of phospholipid-esterified arachidonic acid. They have been used as biomarkers of oxidative stress, but they also have been found to have potent biological activity. ent-8-iso-15(S)-Prostaglandin F2α (ent-8-iso-15(S)-PGF2α) is a potent vasoconstrictor of porcine retinal and brain microvessels with EC50 values of 15 and 24 nM, respectively. This isoprostane is about ten-fold more potent than 8-iso-PGF2α in a whole blood platelet aggregation inhibition assay.
8-iso-13,14-dihydro-15-keto Prostaglandin F2α (8-iso-13,14-dihydro-15-keto PGF2α) is a metabolite of the isoprostane, 8-isoprostane (8-iso PGF2α), in rabbits, monkeys and humans. 8-iso PGF2α is a PG-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-isoprostane is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-isoprostane is infused into rabbits. Early in the infusion (within 10 minutes) 8-iso-13,14-dihydro-15-keto PGF2α was a significant component of the metabolite profile, which was comprised mostly of dinor 8-isoprostane metabolites. 8-iso-13,14-dihydro-15-keto PGF2α weakly inhibits the U-46619 or collagen-induced aggregation of human platelets, although a number of the E-series isoprostanes are much more potent in this assay.
8-iso Prostaglandin F2β (8-iso PGF2β) is an isomer of PGF2α of non-enzymatic 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 does not promote aggregation of human whole blood. However, 8-iso PGF2β moderately contracts both the canine and porcine pulmonary vein, although the effect is much weaker than that exhibited by other isoprostanes such as 8-iso PGE1, 8-iso PGE2, or 8-iso PGF2α. 8-iso-15-keto PGF2β is a potential metabolite of 8-iso PGF2β via the 15-hydroxy PG dehydrogenase pathway. There are no published reports on the formation or biological activity of 8-iso-15-keto PGF2β.
8-iso Prostaglandin E2 (8-iso PGE2) is one of several isoprostanes produced from polyunsaturated fatty acids during lipid peroxidation. 8-iso-16-cyclohexyl-tetranor PGE2 is a synthetic analog of 8-iso PGE2. There are no published studies on the pharmacological properties of 8-iso-16-cyclohexyl-tetranor PGE2.
8-iso-15(R)-Prostaglandin F2α (8-iso-15(R) PGF2α) is a chemically distinct member within a broad group of prostaglandin-like eicosanoids, produced through the free radical peroxidation of arachidonic acid contained in membrane phospholipids. It represents the C-15 epimer of 8-isoPGF2α, distinguished as the sole isoprostane isomer extensively examined across numerous biological systems.
Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker[1].
Mc-O-Si(di-iso)-Cl is a cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs) like Gemcitabine-O-Si(di-iso)-O-Mc [1].
N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs). It serves as a crucial component in the production of Gemcitabine-O-Si(di-iso)-O-Mc, an ADC compound [1].
8-iso Prostaglandin A1 (8-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.
8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the C-1 esters of prostaglandins show greatly diminished agonist activity in vitro compared to the parent free acids.
8-iso PGF3α is an isoprostane produced from the free-radical peroxidation of EPA. Little is known about the biological activity of 8-iso PGF3α. There is one report that it is inactive in a TP receptor mediated assay of human platelet shape change, where 8-iso PGF2α has an ED50 value of 1 uM. [1]
Tunicamycin 14:1 is a mixture of tunicamycin structural isomers that contain a 14-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 14:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) in Streptomyces and directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 14:1 with the iso branching configuration inhibits bacterial phospho-MurNAc-pentapeptide transferase (MraY) with an IC50 value of 0.31 μM.2