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KI3742HPGDS-inhibitor-15 mg$460

Chemical Characteristic

Product NameHPGDS-inhibitor-1
CAS No.1033836-12-2
Molecular Weight 381.37
FormulaC19H19F4N3O
Smilesc1c(ccc(n1)c1cc(ccc1)F)C(=O)NC1CCN(CC1)CC(F)(F)F
Chemical Structure

Biological activities

HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 value of 0.7 nM. HPGDS inhibitor 1 was elected for further profiling based on its enzyme and cell potency. The compound illustrated equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5-2.3 nM). HPGDS inhibitor 1 was profiled in a panel of cellular assays to screen for activity against several relevant human enzyme targets. Oral administration of HPGDS inhibitor 1 blocked PGD2 production in the rat spleen. And the inhibition of PGD2 was inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time and dose-dependent manner. Spleen PGD2 levels fall as HPGDS inhibitor 1 plasma levels increase over time, and PGD2 levels return to baseline levels as HPGDS inhibitor 1 plasma levels decline [1].

References

[1] Chris P. Carron, Trujillo JI, Olson KL, et al. Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS). ACS Med Chem Lett. 2010, 1 (2):59-63

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