[CAS NO. 1337878-62-2] ATI-2341
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PRODUCTS SPECIFICATIONS [1337878-62-2]
Store
Catalog
SLK-S8309
Brand
Selleck
CAS
1337878-62-2
DESCRIPTION [1337878-62-2]
Overview
| MDL | MFCD30182359 |
|---|---|
| Molecular Weight | 2256.82 |
| Molecular Formula | C104H178N26O25S2 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (), 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.
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.
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