Synonym
Leukadherin-1; Leukadherin 1; Leukadherin1; LA1.
IUPAC/Chemical Name
4-[5-[[4-Oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]-benzoic acid
InChi Key
AEZGRQSLKVNPCI-UNOMPAQXSA-N
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-
SMILES Code
O=C(O)C1=CC=C(C2=CC=C(/C=C(SC(N3CC4=CC=CC=C4)=S)/C3=O)O2)C=C1
Purity
>95% (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
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Biological target:
Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM.
In vitro activity:
Leukadherin-1 pretreatment reduces secretion of interferon (IFN)-γ, tumour necrosis factor (TNF) and macrophage inflammatory protein (MIP)-1β by monokine-stimulated NK cells. Leukadherin-1 pretreatment also reduces secretion of IL-1β, IL-6 and TNF by Toll-like receptor (TLR)-2 and TLR-7/8-stimulated monocytes (P < 0·01 for all).
Reference: Clin Exp Immunol. 2016 Sep;185(3):361-71. https://pubmed.ncbi.nlm.nih.gov/27118513/
In vivo activity:
Newborn rats were exposed to normoxia (21% O2) or hyperoxia (85% O2) and received twice-daily intraperitoneal injection of LA1 (leukadherin-1) or placebo for 14 days. Administration of LA1 decreased macrophage infiltration in the lungs during hyperoxia. Furthermore, treatment with LA1 improved alveolarization and angiogenesis and decreased pulmonary vascular remodeling and PH.
Reference: Am J Respir Cell Mol Biol. 2015 Dec;53(6):793-801. https://pubmed.ncbi.nlm.nih.gov/25909334/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
1.0 |
2.37 |
|
| DMSO |
3.7 |
8.70 |
|
| DMSO:PBS (pH 7.2) (1:2) |
0.3 |
0.71 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
421.49
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:
1. Roberts AL, Fürnrohr BG, Vyse TJ, Rhodes B. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016 Sep;185(3):361-71. doi: 10.1111/cei.12803. Epub 2016 Jul 26. PMID: 27118513; PMCID: PMC4991522.
2. Reed JH, Jain M, Lee K, Kandimalla ER, Faridi MH, Buyon JP, Gupta V, Clancy RM. Complement receptor 3 influences toll-like receptor 7/8-dependent inflammation: implications for autoimmune diseases characterized by antibody reactivity to ribonucleoproteins. J Biol Chem. 2013 Mar 29;288(13):9077-83. doi: 10.1074/jbc.M112.403303. Epub 2013 Feb 5. PMID: 23386618; PMCID: PMC3610980.
3. Jagarapu J, Kelchtermans J, Rong M, Chen S, Hehre D, Hummler S, Faridi MH, Gupta V, Wu S. Efficacy of Leukadherin-1 in the Prevention of Hyperoxia-Induced Lung Injury in Neonatal Rats. Am J Respir Cell Mol Biol. 2015 Dec;53(6):793-801. doi: 10.1165/rcmb.2014-0422OC. PMID: 25909334; PMCID: PMC4742935.
4. Khan SQ, Guo L, Cimbaluk DJ, Elshabrawy H, Faridi MH, Jolly M, George JF, Agarwal A, Gupta V. A Small Molecule β2 Integrin Agonist Improves Chronic Kidney Allograft Survival by Reducing Leukocyte Recruitment and Accompanying Vasculopathy. Front Med (Lausanne). 2014 Nov 12;1:45. doi: 10.3389/fmed.2014.00045. PMID: 25593918; PMCID: PMC4291902.
In vitro protocol:
1. Roberts AL, Fürnrohr BG, Vyse TJ, Rhodes B. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016 Sep;185(3):361-71. doi: 10.1111/cei.12803. Epub 2016 Jul 26. PMID: 27118513; PMCID: PMC4991522.
2. Reed JH, Jain M, Lee K, Kandimalla ER, Faridi MH, Buyon JP, Gupta V, Clancy RM. Complement receptor 3 influences toll-like receptor 7/8-dependent inflammation: implications for autoimmune diseases characterized by antibody reactivity to ribonucleoproteins. J Biol Chem. 2013 Mar 29;288(13):9077-83. doi: 10.1074/jbc.M112.403303. Epub 2013 Feb 5. PMID: 23386618; PMCID: PMC3610980.
In vivo protocol:
1. Jagarapu J, Kelchtermans J, Rong M, Chen S, Hehre D, Hummler S, Faridi MH, Gupta V, Wu S. Efficacy of Leukadherin-1 in the Prevention of Hyperoxia-Induced Lung Injury in Neonatal Rats. Am J Respir Cell Mol Biol. 2015 Dec;53(6):793-801. doi: 10.1165/rcmb.2014-0422OC. PMID: 25909334; PMCID: PMC4742935.
2. Khan SQ, Guo L, Cimbaluk DJ, Elshabrawy H, Faridi MH, Jolly M, George JF, Agarwal A, Gupta V. A Small Molecule β2 Integrin Agonist Improves Chronic Kidney Allograft Survival by Reducing Leukocyte Recruitment and Accompanying Vasculopathy. Front Med (Lausanne). 2014 Nov 12;1:45. doi: 10.3389/fmed.2014.00045. PMID: 25593918; PMCID: PMC4291902.
1: Roberts AL, Fürnrohr BG, Vyse TJ, Rhodes B. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016 Sep;185(3):361-71. doi: 10.1111/cei.12803. Epub 2016 Jul 26. PubMed PMID: 27118513; PubMed Central PMCID: PMC4991522.
2: Joshi N, Kopec AK, Ray JL, Cline-Fedewa H, Nawabi A, Schmitt T, Nault R, Zacharewski TR, Rockwell CE, Flick MJ, Luyendyk JP. Fibrin deposition following bile duct injury limits fibrosis through an αMβ2-dependent mechanism. Blood. 2016 Jun 2;127(22):2751-62. doi: 10.1182/blood-2015-09-670703. Epub 2016 Feb 26. PubMed PMID: 26921287; PubMed Central PMCID: PMC4891955.
3: Jagarapu J, Kelchtermans J, Rong M, Chen S, Hehre D, Hummler S, Faridi MH, Gupta V, Wu S. Efficacy of Leukadherin-1 in the Prevention of Hyperoxia-Induced Lung Injury in Neonatal Rats. Am J Respir Cell Mol Biol. 2015 Dec;53(6):793-801. doi: 10.1165/rcmb.2014-0422OC. PubMed PMID: 25909334; PubMed Central PMCID: PMC4742935.
4: Khan SQ, Guo L, Cimbaluk DJ, Elshabrawy H, Faridi MH, Jolly M, George JF, Agarwal A, Gupta V. A Small Molecule β2 Integrin Agonist Improves Chronic Kidney Allograft Survival by Reducing Leukocyte Recruitment and Accompanying Vasculopathy. Front Med (Lausanne). 2014 Nov 12;1:45. doi: 10.3389/fmed.2014.00045. eCollection 2014. PubMed PMID: 25593918; PubMed Central PMCID: PMC4291902.
5: Celik E, Faridi MH, Kumar V, Deep S, Moy VT, Gupta V. Agonist leukadherin-1 increases CD11b/CD18-dependent adhesion via membrane tethers. Biophys J. 2013 Dec 3;105(11):2517-27. doi: 10.1016/j.bpj.2013.10.020. PubMed PMID: 24314082; PubMed Central PMCID: PMC3853324.
