| Identification | Back Directory | [Name]
Leukadherin 1 | [CAS]
344897-95-6 | [Synonyms]
CS-2237
eukadherin-1
Leukadherin 1
Leukadherin-1
Leukadhedrin 1
LA1(Leukadherin-1)
LEUKADHERIN 1;LEUKADHERIN1
4-[5-[[4-Oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-benzoic acid
Benzoic acid, 4-[5-[[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]- | [Molecular Formula]
C22H15NO4S2 | [MDL Number]
MFCD01151276 | [MOL File]
344897-95-6.mol | [Molecular Weight]
421.49 |
| Chemical Properties | Back Directory | [Boiling point ]
634.7±65.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: soluble3mg/mL, clear (warmed) | [form ]
powder | [pka]
4.11±0.10(Predicted) | [color ]
, yellow to orange to brown |
| Hazard Information | Back Directory | [Uses]
Leukadherin 1 is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1 (1). Complement receptor 3 (CR3, CD11b/CD18) is a cell surface receptor expressed on myeloid and natural killer cells (2). | [Biological Activity]
leukadherin 1 is an activator of cd11b/cd18 [1].cd11b/cd18 is a cell surface adhesion receptor that mediates immune functions and leukocyte migration and is expressed primarily in the cells of the innate immune system.leukadherin 1 is a cd11b/cd18 activator. leukadherin 1 increased cd11b/cd18-dependent cell adhesion to fibrinogen with ec50 value of 4 μm [1]. leukadherin 1 increased cd11b/cd18-dependent cell adhesion to its ligand icam-1. in k562 cells, leukadherin 1 increased the binding of cd11b/cd18 to icam-1 through the formation of long membrane tethers [2].in the acute peritonitis mice model, leukadherin 1 significantly reduced neutrophil accumulation by 40% [1]. in a mhc mismatched orthotopic kidney transplantation mouse model, leukadherin 1 reduced interstitial leukocyte infiltration, glomerular damage, neointimal hyperplasia and prolonged survival from 48.5% (csa only) to 100% (csa and la1) [3]. in newborn rats exposed to hyperoxia (85% o2), leukadherin 1 reduced both macrophage and neutrophil infiltration in the lungs [4]. | [in vivo]
Leukadherin-1 (1 mg/kg; i.p.; twice daily for 14 days) is beneficial in preventing hyperoxia-induced neonatal lung injury, an experimental model of bronchopulmonary dysplasia (BPD)[1]. | Animal Model: | Newborn Sprague Dawley rat pups[1] | | Dosage: | 1 mg/kg | | Administration: | I.p.; twice daily for 14 days | | Result: | Beneficial on preventing the lung inflammatory response, improved alveolarization and vascular development, and reduced pulmonary vascular remodeling and PH in a hyperoxia-induced experimental model of BPD. |
| [References]
[1]. maiguel d, faridi mh, wei c, et al. small molecule-mediated activation of the integrin cd11b/cd18 reduces inflammatory disease. sci signal, 2011, 4(189): ra57.
[2]. celik e1, faridi mh, kumar v, et al. agonist leukadherin-1 increases cd11b/cd18-dependent adhesion via membrane tethers. biophys j, 2013, 105(11): 2517-2527.
[3]. khan sq, guo l, cimbaluk dj, et al. a small molecule b2 integrin agonist improves chronic kidney allograft survival by reducing leukocyte recruitment and accompanying vasculopathy. front med (lausanne), 2014, 1: 45.
[4]. jagarapu j, kelchtermans j, rong m, et al. leukadherin-1 attenuates hyperoxia-induced lung injury in neonatal rats. am j respir cell mol biol, 2015. |
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