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.
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- CAS. Nr.: 958860-12-3
- Formel: C35H43N11O7
- Molecular Weight:729.79
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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 Ki 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 300-350 g)[1]
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Dosage:25 mM
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Administration:i.v.; single bolus injection
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Result:Increased circulating endogenous prostaglandin E2 levels to over 200% of vehicle control levels.
Reduced circulating endogenous prostaglandin E2 metabolite levels to 50% of vehicle control levels.
Resulted in 3- to 4-fold higher arterial prostaglandin E2 concentrations after exogenous prostaglandin E2 injection.
Reduced arterial prostaglandin E2 metabolite concentrations to 1/3 to 1/4 of vehicle control levels after exogenous prostaglandin E2 injection.
Chemical Information
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CAS. Nr. 958860-12-3
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Molecular Weight 729.79
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Formel C35H43N11O7
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SMILES
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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
T26A Related Classifications
HY-177440 Related Classifications
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