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ATI-2341 TFA

Catalog No.
B7814
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CXCR4 allosteric agonist
Grouped product items
SizePriceStock Qty
1mg
$126.00
Ship with 10-15 days
5mg
$350.00
Ship with 10-15 days
10mg
$550.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 194 nM

ATI-2341 is a CXCR4 allosteric agonist.

Chemokine CXC-type receptor 4 (CXCR4) and its ligand CXCL12 mediate the retention of polymorphonuclear neutrophils and hematopoietic stem and progenitor cells in the bone marrow. Drugs disrupting CXCL12-mediated chemoattraction of CXCR4-expressing cells are useful for hematopoietic stem and progenitor cells (HSPCs) collection.

In vitro: ATI-2341 could inhibit NKH477-induced cAMP accumulation in CXCR4-HEK cells dose-dependently, but showed no effect in naive HEK-293 parental cells. Pretreatment of CXCR4- HEK cells with pertussis toxin completely abrogated the ability of ATI-2341 to inhibit cAMP accumulation. ATI-2341 could also induce a dose-dependent increase in intracellular calcium in cells transfected with wild-type CXCR4 whereas having no effect on untransfected cells. Activation of such signaling pathway by ATI-2341 was dependent on a fully functional CXCR4 receptor since ATI-2341 was not able to mobilize calcium in cells transfected with a CXCR4 receptor variant [1].

In vivo: ATI-2341 could induce dose-dependent peritoneal recruitment of polymorphonuclear neutrophils (PMNs) when i.p. administered to mice. However, when systemically administered by i.v. bolus, ATI-2341 acted as an antagonist and could dose-dependently mediate release of PMNs from the bone marrow of mice and cynomolgus monkeys. In addition, ATI-2341-mediated release of granulocyte/macrophage progenitor cells from the bone marrow was further confirmed by colony-forming assays [1].

Clinical trial: Up to now, ATI-2341 is still in the preclinical development stage.

Reference:
[1] Tchernychev B et al.  Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells. Proc Natl Acad Sci U S A.2010 Dec 21;107(51):22255-9.

Chemical Properties

StorageStore at -20°C
M.Wt2370.87
Cas No.1337878-62-2 (free base)
FormulaC106H179F3N26O27S2
SolubilitySoluble in DMSO
Chemical Namepalmitoyl-L-methionylglycyl-L-tyrosyl-L-glutaminyl-L-lysyl-L-lysyl-L-leucyl-L-arginyl-L-seryl-L-methionyl-L-threonyl-L-aspartyl-L-lysyl-L-tyrosyl-L-arginyl-L-leucine--2,2,2-trifluoroacetic acid (1/1)
SDFDownload SDF
Canonical SMILESOC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CCCCN)NC([C@@H](NC([C@](NC([C@H](CCSC)NC([C@H](CO)NC([C@@H](NC([C@@H](NC([C@H](CCCCN)NC([C@H](CCCCN)NC([C@@H](NC([C@@H](NC(CNC([C@H](CCSC)NC(CCCCCCCCCCCCCCC)=O)=O)=O)CC1=CC=C(O)C=C1)=O)CCC(N)=O)=O)=O)=O)CC(C)C)=O)CCC
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Sequence

{Pal}-Met-Gly-Tyr-Gln-Lys-Lys-Leu-Arg-Ser-Met-Thr-Asp-Lys-Tyr-Arg-Leu

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

ATI-2341