AH 6809 - CAS 33458-93-4
Catalog number: 33458-93-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H14O5
Molecular Weight:
298.29
COA:
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Targets:
Prostanoid Receptor
Description:
AH 6809 is an EP1 (pA2 = 6.8) and EP2 (Ki = 350 nM) receptor antagonist.
Purity:
≥95.0%
Appearance:
White to off-white Solid
Synonyms:
6-isopropoxy-9-oxoxanthene-2-carboxylic acid
Solubility:
Soluble in DMSO
Storage:
Store at 4 °C
MSDS:
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Application:
An EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
AQFFXPQJLZFABJ-UHFFFAOYSA-N
InChI:
1S/C17H14O5/c1-9(2)21-11-4-5-12-15(8-11)22-14-6-3-10(17(19)20)7-13(14)16(12)18/h3-9H,1-2H3,(H,19,20)
Canonical SMILES:
CC(OC1=CC(OC2=CC=C(C(O)=O)C=C2C3=O)=C3C=C1)C
Current Developer:
Merck
1.Prostanoid receptor expression by human airway smooth muscle cells and regulation of the secretion of granulocyte colony-stimulating factor.
Clarke DL;Belvisi MG;Smith SJ;Hardaker E;Yacoub MH;Meja KK;Newton R;Slater DM;Giembycz MA Am J Physiol Lung Cell Mol Physiol. 2005 Feb;288(2):L238-50.
The prostanoid receptors on human airway smooth muscle cells (HASMC) that augment the release by IL-1beta of granulocyte colony-stimulating factor (G-CSF) have been characterized and the signaling pathway elucidated. PCR of HASM cDNA identified products corresponding to EP(2), EP(3), and EP(4) receptor subtypes. These findings were corroborated at the protein level by immunocytochemistry. IL-1beta promoted the elaboration of G-CSF, which was augmented by PGE(2). Cicaprost (IP receptor agonist) was approximately equiactive with PGE(2), whereas PGD(2), PGF(2alpha), and U-46619 (TP receptor agonist) were over 10-fold less potent. Neither SQ 29,548 nor BW A868C (TP and DP(1) receptor antagonists, respectively) attenuated the enhancement of G-CSF release evoking any of the prostanoids studied. With respect to PGE(2), the EP receptor agonists 16,16-dimethyl PGE(2) (nonselective), misoprostol (EP(2)/EP(3) selective), 17-phenyl-omega-trinor PGE(2) (EP(1) selective), ONO-AE1-259, and butaprost (both EP(2) selective) were full agonists at enhancing G-CSF release. AH 6809 (10 microM) and L-161,982 (2 microM), which can be used in HASMC as selective EP(2) and EP(4) receptor antagonists, respectively, failed to displace to the right the PGE(2) concentration-response curve that described the augmented G-CSF release.
2.Relaxation evoked by extracellular Ca2+ in rat aorta is nerve-independent and involves sarcoplasmic reticulum and L-type Ca2+ channel.
Rocha ML;Bendhack LM Vascul Pharmacol. 2009 Mar-Apr;50(3-4):98-103. doi: 10.1016/j.vph.2008.11.004. Epub 2008 Nov 24.
The perivascular nerve network expresses a Ca2+ receptor that is activated by high extracellular Ca2+ concentrations and causes vasorelaxation in resistance arteries. We have verified the influence of perivascular nerve fibers on the Ca2+-induced relaxation in aortic rings. To test our hypothesis, either pre-contracted aortas isolated from rats after sensory denervation with capsaicin or aortic rings acutely denervated with phenol were stimulated to relax with increasing extracellular Ca2+ concentration. We also studied the role of the endothelium on the Ca2+-induced relaxation, and we verified the participation of endothelial/nonendothelial nitric oxide and cyclooxygenase-arachidonic acid metabolites. Additionally, the role of the sarcoplasmic reticulum, K+ channels and L-type Ca2+ channels on the Ca2+-induced relaxation were evaluated. We have observed that the Ca2+-induced relaxation is completely nerve independent, and it is potentiated by endothelial nitric oxide (NO). In endothelium-denuded aortic rings, indomethacin and AH6809 (PGF2alpha receptor antagonist) enhance the relaxing response to Ca2+. This relaxation is inhibited by thapsigargin and verapamil, while was not altered by tetraethylammonium.
3.Lactoferrin ameliorates prostaglandin E2-mediated inhibition of Na+ -glucose cotransport in enterocytes.
Talukder JR;Griffin A;Jaima A;Boyd B;Wright J Can J Physiol Pharmacol. 2014 Jan;92(1):9-20. doi: 10.1139/cjpp-2013-0211. Epub 2013 Oct 4.
Various immunoinflammatory cytokines are produced during chronic intestinal inflammation, which inhibits Na(+)-glucose cotransport (SGLT1) in villus cells. Lactoferrin (Lf), abundantly present in colostrum, is a multifunctional glycoprotein that is absorbed by receptor-mediated transcytosis in humans and animals and has been shown to exert anti-inflammatory effects. Therefore, this study aimed to examine whether Lf would prevent PGE2 effect on SGLT1 for glucose absorption in enterocytes. Intestinal epithelial cells (IEC-6) were grown on transwell plates, treated with phlorizin, PGE2, AH6809, and Lf, and 3-O-methyl d-glucopyranose (OMG) uptake was measured in 10 days postconfluent. Na(+)-dependent OMG uptake, phlorizin, and immunoblotting studies established the activity and apical membrane localization of SGLT1 in IEC-6 cells. PGE2 inhibited SGLT1 in a concentration- and time-dependent manner with an inhibitory constant (Ki) of 50.0 nmol/L and that was antagonized by prostanoid receptor inhibitor, AH6809. PGE2 did not alter Na(+)/K(+)-ATPase activity. In contrast, quantitative real-time polymerase chain reaction and Western blot analyses revealed that SGLT1-specific transcripts and protein expression level were decreased 3-fold by PGE2.
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CAS 33458-93-4 AH 6809

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