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264275-77-6

264275-77-6 structure
264275-77-6 structure
  • Name: XVA143
  • Chemical Name: XVA143
  • CAS Number: 264275-77-6
  • Molecular Formula: C25H21Cl2N3O8
  • Molecular Weight: 562.36
  • Catalog: Signaling Pathways Cytoskeleton Integrin
  • Create Date: 2021-12-19 09:09:43
  • Modify Date: 2024-01-21 07:14:27
  • XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[1].

Name XVA143
Description XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[1].
Related Catalog
In Vitro XVA143 (1 μM) completely abolishes binding of ICAM-1 to LFA-1 in Mn2+ and Mg2+/EGTA, with no hint of agonism[1].XVA143 restores rolling of the αL-E310A β2 mutant by inducing extension of αL[2]. Cell Viability Assay[1] Cell Line: K562 cells. Concentration: 0, 0.2, 0.5 and 1 μM. Incubation Time: Result: Potent against the weakest activator (2 mM Mg2+/1 mM EGTA, IC50 ~10-3 nM) and least potent against the strongest activator (1 mM Mn2+, IC50 ~10-3 nM). Cell Viability Assay[1] Cell Line: Wild-type murine lymphocytes[1]. Concentration: 100 μM. Incubation Time: Result: Induced a 50% increase in rolling fraction compared to vehicle-treated control cells ((from 27±5% to 41±7%).
References

[1]. Azucena Salas, et al. Rolling adhesion through an extended conformation of integrin alphaLbeta2 and relation to alpha I and beta I-like domain interaction. Immunity. 2004 Apr;20(4):393-406.

[2]. Mélanie R Tardif, et al. LFA-1 antagonists as agents limiting human immunodeficiency virus type 1 infection and transmission and potentiating the effect of the fusion inhibitor T-20. Antimicrob Agents Chemother. 2009 Nov;53(11):4656-66.

Molecular Formula C25H21Cl2N3O8
Molecular Weight 562.36