Lifitegrast - 97%, high purity , Integrin alpha-L/beta-2 (LFA-1) antagonist, CAS No.1025967-78-5, Integrin alpha-L/beta-2 (LFA-1) antagonist

1 Citations
Item Number
L171714
Grouped product items
SKUSizeAvailabilityPrice Qty
L171714-25mg
25mg
In stock
$97.90
L171714-100mg
100mg
In stock
$325.90
L171714-250mg
250mg
In stock
$733.90
L171714-1g
1g
In stock
$2,640.90

LFA-1 (lymphocyte function-associated antigen-1) antagonist

Basic Description

SynonymsEN300-20605731 | 7-hydroxy-2-methyl-3-phenoxy-chromone | CS-6264 | s3714 | A900838 | Q23044263 | N-(2-(1-benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carbonyl)-3-(methanesulfonyl)-L-phenylalanine | (2S)-2-{[2-(1-benzofuran-6-carbon
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsLFA-1 (lymphocyte function-associated antigen-1) antagonist, used to treat ocular vascular complications. Lifitegrast\xa0 is a new type of T cell integrin antagonist designed to mimic the binding epitope of ICAM-1.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionIntegrin alpha-L/beta-2 (LFA-1) antagonist
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

LFA-1 (lymphocyte function-associated antigen-1) antagonist.

Product Properties

ALogP4.7

Associated Targets(Human)

ICAM1 Tchem Intercellular adhesion molecule 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ITGAL Tclin Integrin alpha-L (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ICAM1 Tchem Intercellular adhesion molecule-1 (260 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGAL Tclin Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2 (760 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Salmonella typhimurium (15756 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name (2S)-2-[[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-3,4-dihydro-1H-isoquinoline-6-carbonyl]amino]-3-(3-methylsulfonylphenyl)propanoic acid
INCHI InChI=1S/C29H24Cl2N2O7S/c1-41(38,39)20-4-2-3-16(11-20)12-23(29(36)37)32-27(34)25-22(30)13-19-15-33(9-7-21(19)26(25)31)28(35)18-6-5-17-8-10-40-24(17)14-18/h2-6,8,10-11,13-14,23H,7,9,12,15H2,1H3,(H,32,34)(H,36,37)/t23-/m0/s1
InChi Key JFOZKMSJYSPYLN-QHCPKHFHSA-N
Canonical SMILES CS(=O)(=O)C1=CC=CC(=C1)CC(C(=O)O)NC(=O)C2=C(C=C3CN(CCC3=C2Cl)C(=O)C4=CC5=C(C=C4)C=CO5)Cl
Isomeric SMILES CS(=O)(=O)C1=CC=CC(=C1)C[C@@H](C(=O)O)NC(=O)C2=C(C=C3CN(CCC3=C2Cl)C(=O)C4=CC5=C(C=C4)C=CO5)Cl
PubChem CID 11965427
Molecular Weight 615.48

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

8 results found

Lot NumberCertificate TypeDateItem
I2212040Certificate of AnalysisJun 18, 2024 L171714
I2212041Certificate of AnalysisJun 18, 2024 L171714
I2212042Certificate of AnalysisJun 18, 2024 L171714
I2212046Certificate of AnalysisJun 18, 2024 L171714
L2101362Certificate of AnalysisSep 18, 2023 L171714
L2101363Certificate of AnalysisSep 18, 2023 L171714
L2101364Certificate of AnalysisSep 18, 2023 L171714
L2101366Certificate of AnalysisSep 18, 2023 L171714

Safety and Hazards(GHS)

Pictogram(s) GHS08
Signal Warning
Hazard Statements

H361:Suspected of damaging fertility or the unborn child

Precautionary Statements

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P405:Store locked up.

P501:Dispose of contents/container to ...

P203:Obtain, read and follow all safety instructions before use.

P318:if exposed or concerned, get medical advice.

Related Documents

Citations of This Product

1. Xin Meng, Ye Wang.  (2021)  Drug Repurposing for Influenza Virus Polymerase Acidic (PA) Endonuclease Inhibitor.  MOLECULES,  26  (23): (7326).  [PMID:34885905]

References

1. Giblin PA, Lemieux RM.  (2006)  LFA-1 as a key regulator of immune function: approaches toward the development of LFA-1-based therapeutics..  Curr Pharm Des,  12  (22): (2771-95).  [PMID:16918410]
2. Lam H, Bleiden L, de Paiva CS, Farley W, Stern ME, Pflugfelder SC.  (2009)  Tear cytokine profiles in dysfunctional tear syndrome..  Am J Ophthalmol,  147  (2): (198-205. e1).  [PMID:18992869]
3. Murphy CJ, Bentley E, Miller PE, McIntyre K, Leatherberry G, Dubielzig R, Giuliano E, Moore CP, Phillips TE, Smith PB et al..  (2011)  The pharmacologic assessment of a novel lymphocyte function-associated antigen-1 antagonist (SAR 1118) for the treatment of keratoconjunctivitis sicca in dogs..  Invest Ophthalmol Vis Sci,  52  (6): (3174-80).  [PMID:21330663]
4. Kapp TG, Rechenmacher F, Sobahi TR, Kessler H.  (2013)  Integrin modulators: a patent review..  Expert Opin Ther Pat,  23  (10): (1273-95).  [PMID:24050747]
5. Sheppard JD, Torkildsen GL, Lonsdale JD, D'Ambrosio Jr FA, McLaurin EB, Eiferman RA, Kennedy KS, Semba CP, OPUS-1 Study Group.  (2014)  Lifitegrast ophthalmic solution 5.0% for treatment of dry eye disease: results of the OPUS-1 phase 3 study..  Ophthalmology,  121  (2): (475-83).  [PMID:24289915]
6. Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J et al..  (2012)  Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye..  ACS Med Chem Lett,  (3): (203-6).  [PMID:24900456]
7. A-González N, Castrillo A.  (2011)  Liver X receptors as regulators of macrophage inflammatory and metabolic pathways..  Biochim Biophys Acta,  1812  (8): (982-94).  [PMID:21193033]
8. Xin Meng, Ye Wang.  (2021)  Drug Repurposing for Influenza Virus Polymerase Acidic (PA) Endonuclease Inhibitor.  MOLECULES,  26  (23): (7326).  [PMID:34885905]

Solution Calculators