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. GNF351 (500 nM, 48 hours) significantly reduces the percentage of Ki67-positive cells and cell number after treating proliferating monolayer cultures of human keratinocytes.
|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 ≥ 90 mg/mL|
|Related AhR Products|
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.
CAY10465 is an analog of resveratrol acting as a potent and selective aryl hydrocarbon receptor agonist, with a Ki of 0.2 nM.
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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