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 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.
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.
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AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) with IC50 values of 8nM and 8.2nM for I-IP-10 and I-ITAC, respectively.
SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
AMD-070 is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
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