A 286982
目录号 : GC15192An inhibitor of the LFA-1/ICAM-1 interaction
Cas No.:280749-17-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
A 286982 is a selective inhibitor of LFA-1/ICAM-1 binding and LFA-1 with IC50 value of 44 nM and 35 nM, respectively [1].
Lymphocyte function-associated antigen-1 (LFA-1) is a member of leukocyte intergrins family and involves in T cells binding to antigen presenting cells. Intracellular adhension molecule-1 (ICAM-1) is a type of intercellular adhesion molecule and plays a pivotal role in cell-cell interactions. LFA-1/ICAM-1 interaction plays an important role in the pathogenesis of inflammatory disease [2].
A 286982 is a potent LFA-1/ICAM-1 inhibitor and has a different effect on the binding of compound 2B. When tested with LFA-1/ICAM-1 binding assay and LFA-1-mediated cellular adhesion assays, A-286982 treatment for 28h exhibited inhibition on LFA-1/ICAM-1interaction [1]. Using the LFA-1/ICAM-1 ELISA assay, it was shown that A 286982 exhibited inhibition on the binding of ICAM-1-Ig to LFA-1 by reducing both ligands affinity and binding capacity [3].
References:
[1]. Liu, G., et al., Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead. J Med Chem, 2000. 43(21): p. 4025-40.
[2]. Katakai, T., K. Habiro, and T. Kinashi, Dendritic cells regulate high-speed interstitial T cell migration in the lymph node via LFA-1/ICAM-1. J Immunol, 2013. 191(3): p. 1188-99.
[3]. Keating, S.M., et al., Competition between intercellular adhesion molecule-1 and a small-molecule antagonist for a common binding site on the alphal subunit of lymphocyte function-associated antigen-1. Protein Sci, 2006. 15(2): p. 290-303.
| Cas No. | 280749-17-9 | SDF | |
| 化学名 | (E)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one | ||
| Canonical SMILES | CC(C)C1=CC=CC=C1SC2=C(C=C(C=C2)C=CC(=O)N3CCN(CC3)C(=O)C)[N+](=O)[O-] | ||
| 分子式 | C24H27N3O4S | 分子量 | 453.55 |
| 溶解度 | 30mg/mL in DMSO, or in DMF | 储存条件 | Store at RT |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2048 mL | 11.0241 mL | 22.0483 mL |
| 5 mM | 0.441 mL | 2.2048 mL | 4.4097 mL |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2048 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet