Formulation: A crystalline solid
Formal Name: N-(1-oxohexadecyl)-L-methionylglycyl-L-tyrosyl-L-glutaminyl-L-lysyl-L-lysyl-L-leucyl-L-arginyl-L-seryl-L-methionyl-L-threonyl-L-α-aspartyl-L-lysyl-L-tyrosyl-L-arginyl-L-leucine, trifluoroacetate salt
Purity: ≥98%
Formula Markup: C104H178N26O25S2 • XCF3COOH
Formula Weight: 2256,8
Shelf life (days): 1460
Notes: ATI-2341 is a pepducin Gαi-signaling biased agonist of chemokine (C-X-C motif) receptor 4 (CXCR4).{61067} It induces dissociation of Gαi and Gγ2, indicating activation of Gαi-signaling, with an EC50 value of 0.21 µM in a bioluminescence resonance energy transfer (BRET) assay using HEK293T cells expressing CXCR4. ATI-2341 is selective for Gαi over Gα13 (EC50s = 0.53 and >1 µM, respectively, in BRET engagement assays) and is biased for Gαi engagement over β-arrestin-2, G protein-coupled receptor kinase 2 (GRK2), or GRK3 recruitment, exhibiting bias factor values of 24, 24.9, and 30, respectively. It induces chemotaxis of CCRF-CEM T cells, which endogenously express CXCR4, in a concentration-dependent manner. ATI-2341 (0.45 µmol/kg) increases peritoneal lavage fluid infiltration of polymorphonuclear leukocytes (PMNs) in mice.{61068}
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