Leukadherin 1
目录号 : GC17263
An allosteric activator of CD11b/CD18
Cas No.:344897-95-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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 < 1 month before quantification. To exclude non-specific Leukadherin-1-mediated cytotoxicity, the cell viability is assayed at 24 h using the CellTitre-Glo reagent. No significant loss of viability in comparison with the DMSO control is seen, concurring with published data in other cell types. |
References: [1]. Roberts AL, et al. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016 Sep;185(3):361-71. | |
Leukadherin 1 is an activator of CD11b/CD18 [1].
CD11b/CD18 is a cell surface adhesion receptor that mediates immune functions and leukocyte migration and is expressed primarily in the cells of the innate immune system.
Leukadherin 1 is a CD11b/CD18 activator. Leukadherin 1 increased CD11b/CD18-dependent cell adhesion to fibrinogen with EC50 value of 4 μM [1]. Leukadherin 1 increased CD11b/CD18-dependent cell adhesion to its ligand ICAM-1. In K562 cells, leukadherin 1 increased the binding of CD11b/CD18 to ICAM-1 through the formation of long membrane tethers [2].
In the acute peritonitis mice model, leukadherin 1 significantly reduced neutrophil accumulation by 40% [1]. In a MHC mismatched orthotopic kidney transplantation mouse model, leukadherin 1 reduced interstitial leukocyte infiltration, glomerular damage, neointimal hyperplasia and prolonged survival from 48.5% (CsA only) to 100% (CsA and LA1) [3]. In newborn rats exposed to hyperoxia (85% O2), leukadherin 1 reduced both macrophage and neutrophil infiltration in the lungs [4].
References:
[1]. Maiguel D, Faridi MH, Wei C, et al. Small molecule-mediated activation of the integrin CD11b/CD18 reduces inflammatory disease. Sci Signal, 2011, 4(189): ra57.
[2]. Celik E1, Faridi MH, Kumar V, et al. Agonist leukadherin-1 increases CD11b/CD18-dependent adhesion via membrane tethers. Biophys J, 2013, 105(11): 2517-2527.
[3]. Khan SQ, Guo L, Cimbaluk DJ, et al. A small molecule b2 integrin agonist improves chronic kidney allograft survival by reducing leukocyte recruitment and accompanying vasculopathy. Front Med (Lausanne), 2014, 1: 45.
[4]. Jagarapu J, Kelchtermans J, Rong M, et al. Leukadherin-1 Attenuates Hyperoxia-induced Lung Injury in Neonatal Rats. Am J Respir Cell Mol Biol, 2015.
| Cas No. | 344897-95-6 | SDF | |
| 化学名 | (Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid | ||
| Canonical SMILES | O=C(N(C1=S)CC2=CC=CC=C2)/C(S1)=C([H])/C(O3)=CC=C3C4=CC=C(C(O)=O)C=C4 | ||
| 分子式 | C22H15NO4S2 | 分子量 | 421.49 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。