GSK1325756 (Danirixin) is a non-peptide, high affinity, selective and reversible CXCR2 antagonist (IC50 for CXCL8 = 12.5 nM). GSK1325756 has demonstrated potent antagonism of CXCR2 activity in vitro and anti-inflammatory effects in various preclinical models. Danirixin (GSK1325756) is used for the treatment of chronic obstructive pulmonary disease (COPD).
|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.
Assessment of potential d rug interactions by characterization of human dr ug metabolism pathways using non-invasive bile sampling.
Bloomer JC, et al. Br J Clin Pharmacol. 2013 Feb;75(2):488-96. PMID: 22670830.
|Related CXCR Products|
LY2510924 is a potent and selective CXCR4 antagonist, which blocks SDF-1 binding to CXCR4 with IC50 of 0.079 nM.
Motixafortide (BL-8040) is an antagonist of CXCR4 with IC50 value of 1 nM.
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4).
SX-682 is a potent and selective CXCR1/2 allosteric inhibitor, it may be useful for castration-resistant prostate cancer.
VUF11207 fumarate is a CXCR7 agonist and a high-potency CXCR7 ligand (pKi=8.1).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.