ATI-2341

Catalog No.S8309 Batch:S830901

Technical Data

Formula	C₁₀₄H₁₇₈N₂₆O₂₅S₂
Molecular Weight	2256.82	CAS No.	1337878-62-2
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (44.31 mM)
		Ethanol	2 mg/mL (0.88 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

CXCR4 ^[1]
(in CCRF-CEM cells)

194 nM(EC50)

In vitro

ATI-2341 induces CXCR4- and G protein-dependent signaling, receptor internalization, and chemotaxis in CXCR4-expressing cells. It is the most potent agonist with an EC50 value of 194 ± 16 nM and an intrinsic activity of 81 ± 4%. ATI-2341 is a potent and efficacious mobilizer of bone marrow PMNs(polymorphonuclear neutrophils) and HSPCs(hematopoietic stem and progenitor cells) and could represent a previously undescribed therapeutic approach for the recruitment of HSPCs before ABMT(autologous bone marrow transplantation). ATI-2341 is able to induce chemotaxis of CCRF-CEM cells, inducing the typical bell-shaped curve observed with chemotactic agents^[1].

In vivo

Intraperitoneal (i.p.) injection of ATI-2341 in BALB/c mice results in a dose-dependent recruitment of PMNs into the peritoneum, with a maximal effect seen at 405 nmol/kg. A higher concentration of ATI-2341 results in reduced recruitment, which is reminiscent of the bell-shaped curve generally seen with chemotactic agents. Intravenous (i.v.) administration of ATI-2341 in mice results in a dose-dependent increase in PMNs in the peripheral circulation, measured 90 min after administration of compound. The effect is maximal at 0.66 μmol/kg of ATI-2341. ATI-2341 has no effect on the mobilization of lymphocytes at any dose tested^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HEK-293 cells Concentrations 0, 0.031, 0.125, 0.25, 0.5, 1 μM Incubation Time 30 min 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.
Animal Study:^{^[1]}	Animal Models BALB/c mice Dosages 300 nmol/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
HEK-293 cells
Concentrations
0, 0.031, 0.125, 0.25, 0.5, 1 μM
Incubation Time
30 min
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.

Animal Study:^{^[1]}

Animal Models
BALB/c mice
Dosages
300 nmol/kg
Administration
i.p.

References

[1] Tchernychev B, et al. Proc Natl Acad Sci U S A. 2010, 107(51):22255-9.

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SHIPPING AND STORAGE
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