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Purity: ≥98%
Leukadherin-1, formerly known as LA1, is a novel and specific agonist of Complement receptor 3 (CR3) and the leukocyte surface integrin CD11b/CD18 that enhances leukocyte adhesion to ligands and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Complement receptor 3 (CR3, CD11b/CD18) is a multi-functional receptor expressed predominantly on myeloid and natural killer (NK) cells. Leukadherin-1 (LA1) does not modulate signal transducer and activator of transcription (STAT)-4 phosphorylation. Leukadherin-1 modulates TLR-2 and TLR-7/8-induced monocyte cytokine secretion. Targeting leukocyte trafficking using LA1, an integrin agonist, is beneficial in preventing lung inflammation and protecting alveolar and vascular structures during hyperoxia. Thus, targeting integrin-mediated leukocyte recruitment and inflammation may provide a novel strategy in preventing and treating BPD in preterm infants.
| ln Vitro |
A particular agonist of leukocyte surface integrin CD11b/CD18 (αMβ2; CR3; Mac-1) is leukadherin-1. Monokine-stimulated natural killer (NK) cells secrete less interferon (IFN)-γ, tumor necrosis factor (TNF), and macrophage inflammatory protein (MIP)-1β when pretreated with leukadherin-1. Pretreatment with leukadherin-1 also decreases the release of TNF, IL-1β, and IL-6 by TLR-2 and TLR-7/8 activated monocytes[3].
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| ln Vivo |
In an experimental model of bronchopulmonary dysplasia (BPD), leukadherin-1 (1 mg/kg; ip; twice daily for 14 days) is helpful in preventing hyperoxia-induced neonatal lung injury[1].
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| Enzyme Assay |
Leukadherin-1, also known as LA1, is a novel and specific agonist of Complement receptor 3 (CR3) and the leukocyte surface integrin CD11b/CD18 that enhances leukocyte adhesion to ligands and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Complement receptor 3 (CR3, CD11b/CD18) is a multi-functional receptor expressed predominantly on myeloid and natural killer (NK) cells. Leukadherin-1 (LA1) does not modulate signal transducer and activator of transcription (STAT)-4 phosphorylation. Leukadherin-1 modulates TLR-2 and TLR-7/8-induced monocyte cytokine secretion. Targeting leukocyte trafficking using LA1, an integrin agonist, is beneficial in preventing lung inflammation and protecting alveolar and vascular structures during hyperoxia. Thus, targeting integrin-mediated leukocyte recruitment and inflammation may provide a novel strategy in preventing and treating BPD in preterm infants.
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| Cell Assay |
Supernatant cytokines are quantified after stimulation and culture for 18 h (monocytes) or 24 h (NK cells). Except for bead-based stimulation, all experiments are conducted using 100 µL cells in a 96-well plate format. NK cell stimuli are added as follows: (1) Syk inhibitor (1 μM), (2) Leukadherin-1 or dimethylsulphoxide (DMSO) (vector control) (7.5 μM). Shown to induce∼82% of maximum response with negligible off-target effect, (3) anti-CD210 or isotype control (5 µg/mL), (4) 30-45 min after Leukadherin-1 NK cells are stimulated with combinations of IL-12 (10 ng/mL), IL-15 (30 ng/mL) or IL-18 (10 ng/mL): either IL-12 + IL-15 or IL-12 + IL-18. Monocytes are stimulated using pam3csk4 (TLR-2 agonist, 300 ng/mL) or R848 (TLR-7/8 agonist, 2 µg/mL). Supernatants are stored at −80ºC for .
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| Animal Protocol |
Animal/Disease Models: Newborn Sprague Dawley rat pups[1]
Doses: 1 mg/kg Route of Administration: Ip; twice (two times) daily for 14 days Experimental Results: Beneficial on preventing the lung inflammatory response, improved alveolarization and vascular development, and decreased pulmonary vascular remodeling and PH in a hyperoxia-induced experimental model of BPD. |
| References |
[1]. Jagarapu J, et al. Efficacy of Leukadherin-1 in the Prevention of Hyperoxia-Induced Lung Injury in Neonatal Rats. Am J Respir Cell Mol Biol. 2015;53(6):793-801.
[2]. Maiguel D, et al. Small molecule-mediated activation of the integrin CD11b/CD18 reduces inflammatory disease. Sci Signal. 2011;4(189):ra57. [3]. Roberts AL, et al. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016;185(3):361-371. |
| Molecular Formula |
C22H15NO4S2
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| Molecular Weight |
421.49
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| Exact Mass |
421.0442
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| Elemental Analysis |
C, 62.69; H, 3.59; N, 3.32; O, 15.18; S, 15.21
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| CAS # |
344897-95-6
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| Related CAS # |
(Z)-Leukadherin-1;2055362-72-4;ADH-503;2055362-74-6
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| Appearance |
Solid powder
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| SMILES |
O=C(O)C1=CC=C(C2=CC=C(/C=C(SC(N3CC4=CC=CC=C4)=S)/C3=O)O2)C=C1
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| InChi Key |
AEZGRQSLKVNPCI-UNOMPAQXSA-N
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| InChi Code |
InChI=1S/C22H15NO4S2/c24-20-19(29-22(28)23(20)13-14-4-2-1-3-5-14)12-17-10-11-18(27-17)15-6-8-16(9-7-15)21(25)26/h1-12H,13H2,(H,25,26)/b19-12-
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| Chemical Name |
4-[5-[[4-Oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-benzoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5 mg/mL ( 11.86 mM）
Water: Insoluble Ethanol: Insoluble |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3725 mL | 11.8627 mL | 23.7254 mL | |
| 5 mM | 0.4745 mL | 2.3725 mL | 4.7451 mL | |
| 10 mM | 0.2373 mL | 1.1863 mL | 2.3725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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