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H-PGDS inhibitor 8

Chemical Structure : H-PGDS inhibitor 8

CAS No.: 1033836-12-2

H-PGDS inhibitor 8

Catalog No.: PC-49636Not For Human Use, Lab Use Only.

H-PGDS inhibitor 8 is a potent, selective and orally active hematopoietic prostaglandin D synthase (HPGDS) inhibitor with enzyme IC50 of 0.6 nM, and cell IC50 of 32 nM.

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Biological Activity

H-PGDS inhibitor 8 is a potent, selective and orally active hematopoietic prostaglandin D synthase (HPGDS) inhibitor with enzyme IC50 of 0.6 nM, and cell IC50 of 32 nM.
H-PGDS inhibitor 8 exhibitd equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5−2.3 nM).
H-PGDS inhibitor 8 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5 LOX (IC50 values > 10000 nM).
Oral administration of H-PGDS inhibitor 8 (10 mpk) blocked PGD2 production in the rat spleen.
H-PGDS inhibitor 8 (1 mg/mL) completely prevented the LAR (maximum was 86% inhibition of LAR) and blocked the AHR (no change in post antigen PC400) in a model of antigen-induced airway response in allergic sheep.

Physicochemical Properties

M.Wt 381.37
Formula C19H19F4N3O
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

6-(3-fluorophenyl)-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)nicotinamide

References

1. Chris P Carron, et al. ACS Med Chem Lett. 2010 Feb 2;1(2):59-63.

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