ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4). ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
|Cell lines||HEK-293 cells|
|Preparation method||Receptors(CXCR4-eGFP) are transiently transfected into HEK-293 cells and are plated 24 h after transfection on glass coverslips coated with poly-D-lysine. The next day, cells are treated with either vehicle alone or with varying concentrations of ATI-2341 for 30 min at 37 °C followed by fixation with methanol for 5 min at -20 °C. GFP fluorescence is visualized directly using a Zeiss Axiovert inverted microscope. Images are processed using Adobe Photoshop and Adobe Illustrator.|
|Concentrations||0, 0.031, 0.125, 0.25, 0.5, 1 μM|
|Incubation time||30 min|
|Animal models||BALB/c mice|
|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.
|CAS Number||1337878-62-2 (free base)|
|Solubility||DMSO 100 mg/mL|
Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein
Julie Quoyer, et al. Proc Natl Acad Sci U S A. 2013 Dec 24;110(52):E5088-97. PMID: 24309376.
Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells
Boris Tchernychev, et al. Proc Natl Acad Sci U S A. 2010 Dec 21;107(51):22255-9. PMID: 21139054.
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