MDK36122 selectively blocks HPGDS (IC50s = 0.7 and 32 nM in enzyme and cellular assays, respectively) with little activity against the related human enzymes L-PGDS, mPGES, COX-1, COX-2, and 5-LOX.
Oral administration of HPGDS inhibitor 1 blocked PGD2 production in the rat spleen; 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; PGD2 levels return to baseline levels as HPGDS inhibitor 1 plasma levels decline.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).
Carron CP, et al. ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. PMID: 24900177.
Dithiothreitol (DTT) is the common name for a small-molecule redox reagent known as Cleland's reagent; as a reducing or "deprotecting" agent for thiolated DNA.
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.
FICZ is a potent aryl hydrogen receptor (AhR) agonist.
NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
STING-Inducer-1 (ML RR-S2 CDA) is an inducer of STING (stimulator of interferon genes).
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