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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 Experiment | |
|---|---|
| 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 Experiment | |
|---|---|
| Animal models | BALB/c mice |
| Formulation | - |
| Dosages | 300 nmol/kg |
| Administration | i.p. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Molecular Weight | 2370.84 |
| Formula | C106H179F3N26O27S2 |
| CAS Number | 1337878-62-2 (free base) |
| Purity | >98% |
| Solubility | DMSO 100 mg/mL |
| Storage | -20°C, sealed |
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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