XVA143

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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.

For research use only. We do not sell to patients.

XVA143 Chemical Structure

CAS No. : 264275-77-6

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•Related Small Molecules:

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View All Isoforms

αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

Biological Activity
Purity & Documentation
References
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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].

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 α_L-E310A β₂ mutant by inducing extension of α_L^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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%).

Molecular Weight

562.36

Formula

C₂₅H₂₁Cl₂N₃O₈

CAS No.

264275-77-6

SMILES

O=C(O)[C@H](CNC(C1=CC(O)=CC(O)=C1)=O)NC(C2=C(Cl)C=C(C(NCC3=CC=CC(O)=C3)=O)C=C2Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

XVA143 Related Classifications

Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XVA143264275-77-6XVA 143XVA-143IntegrinICAM-1EGTALFA-1α/β IintegrinHIVInhibitorinhibitorinhibit

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