CAY10465 is an analog of resveratrol acting as a potent and selective aryl hydrocarbon receptor agonist, with a Ki of 0.2 nM. CAY10465 is inactive as a ligand for the estrogen receptor even at 100 µM. CAY10465 (0.01 nM-100 μM) reduces apolipoprotein A-I (apo A-I) levels in HepG2 cells, and inhibits the synthesis of the protein.
|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 ≥ 65 mg/mL|
Inhibition of apolipoprotein A-I gene by the aryl hydrocarbon receptor: a potential mechanism for smoking-associated hypoalphalipoproteinemia
Emad Naem, et al. Life Sci. 2012 Jul 26;91(1-2):64-9. PMID: 22727790.
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators
Philippe de Medina, et al. J Med Chem. 2005 Jan 13;48(1):287-91. PMID: 15634023.
|Related AhR Products|
GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM.
D-kynurenine is a metabolite of D-tryptophan, which can be used as a biological precursor of KYNA and 3-hydroxykynurenine.
L-Kynurenine is an aryl hydrocarbon receptor agonist.
PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist, with a Ki of 1.2 nM.
YL-109 is a novel anticancer agent, which can inhibit breast cancer cell growth and invasiveness in vitro and in vivo, YL-109 is also an STUB1 enhancer.
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