WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H208223
CAS#: 264275-77-6
Description: XVA143 is a α/β I allosteric inhibitor of the integrin leucocyte function-associated antigen-1 (αLβ2, LFA-1) which plays crucial roles in T cell adhesion, migration and immunological synapse (IS) formation. Consequently, αLβ2 is an important therapeutic target in autoimmunity.
Hodoodo Cat#: H208223
Name: XVA143
CAS#: 264275-77-6
Chemical Formula: C25H21Cl2N3O8
Exact Mass: 561.07
Molecular Weight: 562.340
Elemental Analysis: C, 53.40; H, 3.76; Cl, 12.61; N, 7.47; O, 22.76
This product is not in stock, which may be available by custom synthesis.
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Synonym: XVA-143, XV-A143, XVA1-43
IUPAC/Chemical Name: (2S)-2-[[2,6-Dichloro-4-[(3-hydroxyphenyl)methylcarbamoyl]benzoyl]amino]-3-[(3,5-dihydroxybenzoyl)amino]propanoic acid
InChi Key: FZKFBGXSXUYBMX-FQEVSTJZSA-N
InChi Code: InChI=1S/C25H21Cl2N3O8/c26-18-7-14(23(35)28-10-12-2-1-3-15(31)4-12)8-19(27)21(18)24(36)30-20(25(37)38)11-29-22(34)13-5-16(32)9-17(33)6-13/h1-9,20,31-33H,10-11H2,(H,28,35)(H,29,34)(H,30,36)(H,37,38)/t20-/m0/s1
SMILES Code: OC1=CC(C(NC[C@H](NC(C2=C(Cl)C=C(C(NCC3=CC(O)=CC=C3)=O)C=C2Cl)=O)C(O)=O)=O)=CC(O)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 562.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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5: Parmley LA, Elkins ND, Fini MA, Liu YE, Repine JE, Wright RM. Alpha-4/beta-1 and alpha-L/beta-2 integrins mediate cytokine induced lung leukocyte-epithelial adhesion and injury. Br J Pharmacol. 2007 Nov;152(6):915-29. doi: 10.1038/sj.bjp.0707443. Epub 2007 Sep 10. PMID: 17828290; PMCID: PMC2078224.
6: Wilson ZS, Ahn LB, Serratelli WS, Belley MD, Lomas-Neira J, Sen M, Lefort CT. Activated β2 Integrins Restrict Neutrophil Recruitment during Murine Acute Pseudomonal Pneumonia. Am J Respir Cell Mol Biol. 2017 May;56(5):620-627. doi: 10.1165/rcmb.2016-0215OC. PMID: 28157452; PMCID: PMC5449489.
7: Hajishengallis G, McIntosh ML, Nishiyama SI, Yoshimura F. Mechanism and implications of CXCR4-mediated integrin activation by Porphyromonas gingivalis. Mol Oral Microbiol. 2013 Aug;28(4):239-49. doi: 10.1111/omi.12021. Epub 2013 Jan 21. PMID: 23331495; PMCID: PMC4123224.
8: Xiang X, Lee CY, Li T, Chen W, Lou J, Zhu C. Structural basis and kinetics of force-induced conformational changes of an αA domain-containing integrin. PLoS One. 2011;6(11):e27946. doi: 10.1371/journal.pone.0027946. Epub 2011 Nov 28. PMID: 22140490; PMCID: PMC3225382.
9: Chen W, Lou J, Zhu C. Forcing switch from short- to intermediate- and long- lived states of the alphaA domain generates LFA-1/ICAM-1 catch bonds. J Biol Chem. 2010 Nov 12;285(46):35967-78. doi: 10.1074/jbc.M110.155770. Epub 2010 Sep 6. Erratum in: J Biol Chem. 2011 May 20;286(20):18344. PMID: 20819952; PMCID: PMC2975219.
10: Tardif MR, Gilbert C, Thibault S, Fortin JF, Tremblay MJ. 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. doi: 10.1128/AAC.00117-09. Epub 2009 Aug 31. PMID: 19721069; PMCID: PMC2772324.