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Leukadherin-1 Integrin agonist

Name: Leukadherin-1
Brand: Selleck Chemicals
SKU: S8306
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8306

Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1 (an agonist for the complement receptor 3 (CD11b/CD18)).

Chemical Structure

Molecular Weight: 421.49

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S830601 DMSO]5 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.86%

99.86

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Chemical Information, Storage & Stability

Molecular Weight	421.49	Formula	C₂₂H₁₅NO₄S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	344897-95-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)CN2C(=O)C(=CC3=CC=C(O3)C4=CC=C(C=C4)C(=O)O)SC2=S

Solubility

In vitro
Batch:

DMSO : 5 mg/mL ( (11.86 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.125mg/ml (0.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 2.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CD11b/CD18 ^[3]
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. This compound modulates NK cell cytokine secretion and does not modulate Syk activation in NK cells^[1]. 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^[3].
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^[1]. This compound increases leukocyte adhesion, preventing their transmigration and tissue recruitment in vivo. This chemical 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^[2].
References	https://pubmed.ncbi.nlm.nih.gov/27118513/ https://pubmed.ncbi.nlm.nih.gov/25593918/ https://pubmed.ncbi.nlm.nih.gov/21900205/

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