XVA143
Based on 1 Customer Validation
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.
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- Pureté: 99.94%
- CAS No.: 264275-77-6
- Formule: C25H21Cl2N3O8
- Masse moléculaire:562.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells.
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Concentration:0, 0.2, 0.5 and 1 μM.
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Incubation Time:
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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).
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Cell Line:Wild-type murine lymphocytes[1].
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Concentration:100 μM.
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Incubation Time:
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Result:Induced a 50% increase in rolling fraction compared to vehicle-treated control cells ((from 27±5% to 41±7%).
Chemical Information
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CAS No. 264275-77-6
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Appearance Solid
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Masse moléculaire 562.36
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Formule C25H21Cl2N3O8
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (177.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7782 mL | 8.8911 mL | 17.7822 mL | 44.4555 mL |
| 5 mM | 0.3556 mL | 1.7782 mL | 3.5564 mL | 8.8911 mL | |
| 10 mM | 0.1778 mL | 0.8891 mL | 1.7782 mL | 4.4456 mL | |
| 15 mM | 0.1185 mL | 0.5927 mL | 1.1855 mL | 2.9637 mL | |
| 20 mM | 0.0889 mL | 0.4446 mL | 0.8891 mL | 2.2228 mL | |
| 25 mM | 0.0711 mL | 0.3556 mL | 0.7113 mL | 1.7782 mL | |
| 30 mM | 0.0593 mL | 0.2964 mL | 0.5927 mL | 1.4819 mL | |
| 40 mM | 0.0445 mL | 0.2223 mL | 0.4446 mL | 1.1114 mL | |
| 50 mM | 0.0356 mL | 0.1778 mL | 0.3556 mL | 0.8891 mL | |
| 60 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7409 mL | |
| 80 mM | 0.0222 mL | 0.1111 mL | 0.2223 mL | 0.5557 mL | |
| 100 mM | 0.0178 mL | 0.0889 mL | 0.1778 mL | 0.4446 mL |