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.
|all-trans 4-Keto Retinoic Acid
all-trans 4-Keto Retinoic Acid is an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
GK921 is a transglutaminase 2 (TGase 2) inhibitor.
Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
Aramchol is a cholesterol solubilizer that prevents gallstone formation in inbred mice.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.