Leukadherin-1

SKU: orb1303971

Description

Leukadherin-1 is a small molecule allosteric activator of the integrin CD11b/CD18 (Mac-1). It promotes CD11b-dependent adhesion to ligands like fibrinogen while inhibiting leukocyte migration, making it a valuable research tool for studying inflammation in both cellular and animal models.

Research Area

Immunology & Inflammation, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	344897-95-6
MW	421.49
Purity	98.49% (May vary between batches)
Formula	C₂₂H₁₅NO₄S₂
SMILES	OC(=O)c1ccc(cc1)-c1ccc(\C=C2/SC(=S)N(Cc3ccccc3)C2=O)o1
Target	Complement System\|\|\|Integrin
Solubility	H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:15 mg/mL (35.59 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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In Vivo	Leukadherin-1 has potent anti-inflammatory effects in a range of animal models, including an autoimmune nephritis model, without obvious short-term side effects. Leukadherin-1 (LA1) increases leukocyte adhesion, preventing their transmigration and tissue recruitment in vivo. LA1 treatment reduces interstitial leukocyte infiltration in the allograft, reduces neointimal hyperplasia and glomerular damage, and prolongs graft survival from 48.5% (CsA only) to 100% (CsA and LA1) on day 60 in a mouse model of fully MHC-mismatched orthotopic kidney transplantation.
In Vitro	Leukadherin-1 pretreatment reduces secretion of interferon (IFN)-γ, tumour necrosis factor (TNF) and macrophage inflammatory protein (MIP)-1β by monokine-stimulated NK cells. It also reduces secretion of IL-1β, IL-6 and TNF by Toll-like receptor (TLR)-2 and TLR-7/8-stimulated monocytes. Leukadherin-1 modulates NK cell cytokine secretion and does not modulate Syk activation in NK cells. LA1 increases CD11b/CD18-dependent cell adhesion to fibrinogen with 50% effective concentration (EC50, the effective concentration for a 50% increase in adhesion) values of 4 μM.
Cell Research	NK cell stimuli (where used) were 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 were 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 were stimulated using pam3csk4 (TLR-2 agonist, 300 ng/ml) or R848 (TLR-7/8 agonist, 2 µg/ml). Supernatants were stored at −80ºC for < 1 month before quantification. To exclude non-specific Leukadherin-1-mediated cytotoxicity, cell viability is assessed at 24 h using the CellTitre-Glo reagent. (Only for Reference)

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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endothelium, ICAM-1, Inhibitor, Integrin, Leukadherin 1, Leukadherin1, Leukadherin-1, leukocyte, inhibit, inflammatory, Mac-1, CR3, Complement System, ComplementSystem, CD11b/CD18, adhesion, vascular, αMβ2

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Compound Identifiers

PubChem CID

5342077 ↗

Key Properties

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No computed properties available.

Protocol Information

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CAS Number:	2055362-72-4
MW:	421.49
Formula:	C₂₂H₁₅NO₄S₂

Purity:	>98% (HPLC)
CAS Number:	344897-95-6
MW:	421.49
Formula:	C₂₂H₁₅NO₄S₂

Leukadherin-1

Description

Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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