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HQL-79

Chemical Structure : HQL-79

CAS No.: 162641-16-9

HQL-79 (HQL79)

Catalog No.: PC-49639Not For Human Use, Lab Use Only.

HQL-79 (HQL79) is an orally selective inhibitor of human hematopoietic prostaglandin D synthase (H-PGDS), inhibits human H-PGDS competitively against the substrate PGH2 and non-competitively against GSH with Ki of 5 and 3 uM, respectively.

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Biological Activity

HQL-79 (HQL79) is an orally selective inhibitor of human hematopoietic prostaglandin D synthase (H-PGDS), inhibits human H-PGDS competitively against the substrate PGH2 and non-competitively against GSH with Ki of 5 and 3 uM, respectively.
HQL-79 binds to H-PGDS with an affinity that is 12-fold higher in the presence of GSH and Mg2+ (Kd, 0.8 uM) than in their absence.
HQL-79 selectively inhibited PGD2 production by H-PGDS-expressing human megakaryocytes and rat mastocytoma cells with an IC50 value of about 100 uM but only marginally affected the production of other prostanoids.
Orally administered HQL-79 (30 mg/kg body weight) inhibited antigen-induced production of PGD2, without affecting the production of PGE2 and PGF2alpha, and ameliorated airway inflammation in wild-type and human H-PGDS-overexpressing mice.

Physicochemical Properties

M.Wt 377.48
Formula C22H27N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(Diphenylmethoxy)-1-[3-(2H-tetrazol-5-yl)propyl]piperidine

References

1. Aritake K, et al. J Biol Chem. 2006 Jun 2;281(22):15277-86.

2. Tajima T, et al. J Pharmacol Exp Ther. 2008 Aug;326(2):493-501.

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