For research use only. Not for therapeutic Use.
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect[1][2][3].
LXW7 specially binds to αvβ3 integrin (Kd=76±10 nM). LXW7 binds strongly to αvβ3-K562 cells, weakly to αvβ5-K562 cells and αIIbβ3-K562 cells, and no binding to K562 cells. LXW7 has great potential as a highly efficient peptide ligand for targeted imaging and drug delivery[1].
LXW7 acts as a potent and specific endothelial progenitor cells (EPCs) and endothelial cells (ECs) targeting ligand[2].
LXW7 (100 μg/kg; intravenous injection) significantly lowers infarct volumes and brain water content (BWC) LXW7-treated rats. The LXW7 treatment lowers the expression of pro-inflammatory cytokines[3].
Catalog Number | I045902 |
Synonyms | 2-[(4S,7R,10R,13S,19S,25S)-25-amino-4-carbamoyl-10-(carboxymethyl)-19-[3-(diaminomethylideneamino)propyl]-6,9,12,15,18,21,24-heptaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacos-13-yl]acetic acid;2,2,2-trifluoroacetic acid |
Molecular Formula | C31H49F3N12O14S2 |
Purity | ≥95% |
InChI | InChI=1S/C29H48N12O12S2.C2HF3O2/c1-12(2)22-28(53)40-17(23(31)48)11-55-54-10-13(30)24(49)35-8-18(42)37-14(4-3-5-34-29(32)33)25(50)36-9-19(43)38-15(6-20(44)45)26(51)39-16(7-21(46)47)27(52)41-22;3-2(4,5)1(6)7/h12-17,22H,3-11,30H2,1-2H3,(H2,31,48)(H,35,49)(H,36,50)(H,37,42)(H,38,43)(H,39,51)(H,40,53)(H,41,52)(H,44,45)(H,46,47)(H4,32,33,34);(H,6,7)/t13-,14+,15+,16-,17-,22-;/m1./s1 |
InChIKey | CABFZTZDDADZJM-XXKHBVEGSA-N |
SMILES | CC(C)C1C(=O)NC(CSSCC(C(=O)NCC(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1)CC(=O)O)CC(=O)O)CCCN=C(N)N)N)C(=O)N.C(=O)(C(F)(F)F)O |
Reference | [1]. Xiao W, et al. The use of one-bead one-compound combinatorial library technology to discover high-affinity αvβ3 integrin and cancer targeting arginine-glycine-aspartic acid ligands with a built-in handle. Mol Cancer Ther. 2010 Oct;9(10):2714-23. [2]. Hao D, et al. Discovery and Characterization of a Potent and Specific Peptide Ligand Targeting Endothelial Progenitor Cells and Endothelial Cells for Tissue Regeneration. ACS Chem Biol. 2017 Apr 21;12(4):1075-1086. [3]. Fang T, et al. LXW7 ameliorates focal cerebral ischemia injury and attenuates inflammatory responses in activated microglia in rats. Braz J Med Biol Res. 2016 Aug 1;49(9):e5287. |