LY518674 is a potent and selective PPAR-alpha antagonist with EC50 of 42 nM for human PPARα. LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndrome. LY518674 produced a dose-dependent increase in serum HDL-c, resulting in 208 +/- 15% elevation at optimum dose. In cultured hepatocytes, LY518674 produced 50% higher apoA-1 secretion, which was associated with increase in radiolabeled methionine incorporation in apoA-1.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 100 mg/mL|
|Related PPAR Products|
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
GW1929 is a potent PPAR-γ agonist, with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively.
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2.
NXT629 is an effective, selective and competitive PPAR-α antagonist. The IC50 value of HUMAN PPARα is 77 nM, which is higher than that of other nuclear hormone receptors, such as PPARδ, PPARγ, Erβ, GR and TRβ, with IC50 value of 6.0, 15, respectively. 15.2, 32.5 and >100 μM.
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a PPARγ agonist with high affinity, activity dependent on PPARγ, inhibiting growth, IC50 is 0.8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.