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ATI-2341 TFA

Cat. No. M10141
ATI-2341 TFA Structure
Size Price Availability Quantity
1mg USD 140  USD140 In stock
5mg USD 380  USD380 In stock
10mg USD 590  USD590 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 2370.84
Formula C106H179F3N26O27S2
CAS Number 1337878-62-2 (free base)
Purity >98%
Solubility DMSO 100 mg/mL
Storage -20°C, sealed
References

[1] Julie Quoyer, et al. Proc Natl Acad Sci U S A. Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein

[2] Boris Tchernychev, et al. Proc Natl Acad Sci U S A. Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells

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ATI-2341

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

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