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HQL-79 is a selective inhibtor of hematopoietic prostaglandin D (PGD) synthase, one of two synthases involved in the production of Prostaglandin D2 (PGD2) from arachidonic acid. HQL-79 selectively inhibited the activity of recombinant H-PGDS with an IC50 of 6 μM and had almost no effect on COX-1, COX-2, m-PGES, or L-PGDS up to 300 μM. HQL-79 has anti-inflammatory activity in vitro and in vivo. HQL-79 is antiallergic and anti-inflammatory. HQL-79 displays antiasthmatic activity and potent antihistaminic properties in vivo. HQL-79 is a synthetic tetrazole compound originally prepared as a possible antihistamine. Subsequent evaluation in models of allergy and asthma demonstrates the HQL-79 inhibits the synthesis of PGD2. HQL-79 is thus a likely lead compound for the preparation of potent, selective PGE synthase inhibitors.
| Molecular Weight | 377.48 |
| Formula | C22H27N5O |
| CAS Number | 162641-16-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PGE synthase Products |
|---|
| Vipoglanstat
Vipoglanstat (BI 1029539) is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = ≤0.5 nM in isolated human whole blood). Vipoglanstat reduces LPS-induced increases in the influx of neutrophils and levels of cytokines in bronchoalveolar lavage fluid (BALF), as well as the expression of PTGES, the gene encoding mPGES-1, Cox2, and Icam1 in the lung parenchyma, in a human PTGES knock-in mouse model of acute lung injury when administered at a dose of 30 mg/kg. |
| mPGES1-IN-7
mPGES-1-IN-2 is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). |
| (E)-KME-4
(E)-KME-4 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM. |
| Friluglanstat
Friluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor, with anti-inflammatory activity. |
| UT-11
UT-11 is a potent and brain-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor. |
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