Leukadherin-1

製品コードS8306 バッチS830601

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₁₅NO₄S₂

分子量

421.49

CAS No.

344897-95-6

Solubility (25°C)*

体外

DMSO

5 mg/mL (11.86 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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)).
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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NK cells
	濃度	7.5 μM
	反応時間	30-45 min
	実験の流れ	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 this compound 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 this chemical-mediated cytotoxicity, cell viability is assessed at 24 h using the CellTitre-Glo reagent.
動物実験	動物モデル	Male C57BL/6J (H-2b) and Balb/cJ (H-2d) mice
	投薬量	1 mg/kg or 2.5 mg/kg
	投与方法	i.v or i.p

参考

https://pubmed.ncbi.nlm.nih.gov/27118513/
https://pubmed.ncbi.nlm.nih.gov/25593918/
https://pubmed.ncbi.nlm.nih.gov/21900205/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Leukadherin-1 inhibits NLRP3 inflammasome by blocking inflammasome assembly [ International Immunopharmacology, 2023, Volume 118]	PubMed: None
Leukadherin-1 inhibits NLRP3 inflammasome by blocking inflammasome assembly [ Int Immunopharmacol, 2023, 118:110024]	PubMed: 36958209
Role of complement C1q/C3-CR3 signaling in brain injury after experimental intracerebral hemorrhage and the effect of minocycline treatment [ Front Immunol, 2022, 13:919444]	PubMed: 36189326
Microglial Activation Mediates Noradrenergic Locus Coeruleus Neurodegeneration via Complement Receptor 3 in a Rotenone-Induced Parkinson's Disease Mouse Model [ J Inflamm Res, 2021, 14:1341-1356]	PubMed: 33859489
Endothelial Progenitor Cell Transplantation Attenuated Synaptic Loss by Enhancing CR3 Dependent Microglial Phagocytosis in Mice [ Research Square, 2021, 10.21203/rs.3.rs-870799/v1]	PubMed: None
Pharmacologic manipulation of complement receptor 3 prevents dendritic spine loss and cognitive impairment after acute cranial radiation [ bioRxiv, 2020, 10.1101/2020.11.25.398701]	PubMed: None
Leukadherin-1-Mediated Activation of CD11b Inhibits LPS-Induced Pro-inflammatory Response in Macrophages and Protects Mice Against Endotoxic Shock by Blocking LPS-TLR4 Interaction [ Front Immunol, 2019, 10:215]	PubMed: 30809230

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。