T26A 

T26A is a highly selective prostaglandin transporter (PGT) inhibitor.T26A does not interact with the PGT homolog OATPc, blocks PGT-mediated PGE₂ influx, and blocks PGE₂ metabolism.T26A retains PGE₂ in the extracellular compartment and reduces intracellular PGE₂ metabolites.T26A elevates circulating endogenous PGE₂ levels, reduces circulating endogenous PGE₂ metabolite levels, and slows metabolism of exogenously injected PGE₂ in Rattus norvegicus via intravenous injection.T26A does not affect PGE₂ synthesis.T26A can be used for the research of PGT function in adult animals^[1].

T26A (5 μM; 10 min) inhibits 94% of PGT-mediated [³H]PGE₂ uptake in PGT-MDCK cells^[1].
T26A (500-1000 nM; 2 min) acts as a competitive inhibitor of PGT in PGT-MDCK cells, with a K_i of 378 nM^[1].
T26A (0.5-50 μM) exerts no significant effect on the activity of purified ovine COX1, ovine COX2 or human recombinant COX2 enzymes; it also shows no significant effect on the activity of purified human recombinant m-PGES enzyme^[1].
T26A (5 μM) has no effect on the synthesis and release of PGE₂ in WT-MDCK cells treated with 1 μM arachidonic acid (HY-109590) for different durations^[1].
T26A (5 μM; 10-180 min) blocks PGT-mediated influx and metabolism of endogenous PGE₂ in PGT-MDCK cells, maintains extracellular PGE₂ at the level observed in WT-MDCK cells, and reduces the levels of intracellular PGE₂ metabolites^[1].
T26A (5 μM; 10-180 min) abolishes PGT-mediated metabolism of exogenous 10 nM PGE₂ in PGT-MDCK cells, allowing extracellular PGE₂ to persist and reducing intracellular PGE₂ metabolites^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

T26A (25 mM; i.v.; single dose) increases the level of endogenous circulating prostaglandin E₂, reduces the level of endogenous prostaglandin E₂ metabolites, and slows down the metabolism of exogenously administered prostaglandin E₂ in rats, ultimately leading to elevated circulating prostaglandin E₂ levels in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

729.79

C₃₅H₄₃N₁₁O₇

958860-12-3

O=C(NCCOCCOCCN=[N+]=[N-])C1=CC=C(NC2=NC(NCCOCCOCCNC(C3=CC=CC=C3)=O)=NC(NC4=CC=C(O)C=C4)=N2)C=C1

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• [1]. Chi Y, et al. Development of a high-affinity inhibitor of the prostaglandin transporter. J Pharmacol Exp Ther. 2011;339(2):633-641.  [Content Brief]