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ML401 Sale

目录号 : GC38820

ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.

ML401 Chemical Structure

Cas No.:1597489-14-9

规格 价格 库存 购买数量
1mg
¥926.00
现货
5mg
¥2,700.00
现货
10mg
¥4,320.00
现货
25mg
¥7,920.00
现货
50mg
¥12,150.00
现货
100mg
¥17,357.00
现货
200mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

ML401, a potent chemical probe, selectively antagonizes G-protein coupled receptor 183 (GPR183, EBI2) with an IC50 of 1.03 nM, and displays activity in a chemotaxis assay with IC50 of 6.24 nM.

[1] Ardecky R, et al. 2014 Apr 15 [updated 2015 Jan 16]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–.

Chemical Properties

Cas No. 1597489-14-9 SDF
Canonical SMILES O=C(/C=C/C1=CC=C(C=C1)Br)N2CCN(CC2)CC3=CC=C(C=C3)Cl
分子式 C20H20BrClN2O 分子量 419.74
溶解度 DMSO: 10.42 mg/mL (24.82 mM) 储存条件 Store at -20°C
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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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3824 mL 11.9121 mL 23.8243 mL
5 mM 0.4765 mL 2.3824 mL 4.7649 mL
10 mM 0.2382 mL 1.1912 mL 2.3824 mL
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Research Update

Functional Antagonists of EBI-2

PMID:25834900DOI:NBK280046

A robust antibody response is essential for efficient identification and eradication of pathogenic microbes and toxins, whereas dysregulation of the antibody response can lead to autoimmune disease. Specific antigen encounter by B lymphocytes induces clonal expansion that encompasses several distinct stages of differentiation. During this differentiation process, a critical cell fate decision is made wherein some B cells will undergo terminal differentiation into antibody-producing cells, while a separate cohort will assume a distinct pathway of differentiation to become long-lived memory B cells. An exciting new development in the field is the revelation of a novel chemotactic axis involving the recognition of oxysterol compounds by the orphan G-protein-coupled receptor (GPCR), Epstein-Barr virus-induced gene 2 (EBI2). EBI2 is expressed on B cells and is highly induced upon activation. Recent gene targeting experiments revealed that EBI2-/- B cells exhibited defective migration, resulting in strongly impaired T cell-dependent antibody responses. Most recently, two research teams made the unlikely discovery that oxysterol compounds, previously known to bind nuclear receptors, are the physiologic ligands for EBI2. In order to investigate the importance of EBI2 in immune processes and potential as a drug target, selective and potent antagonists with good in vivo pharmacokinetics need to be developed. This probe report describes a potent functional antagonist of EBI-2, ML401 (CID 73169083, SID 173333998), which is potent (IC50 ∼ 1 nM), displays activity in a chemotaxis assay (IC50 ∼ 6 nM), and has a clean profile in a Eurofins/Ricerca panel as well as excellent rodent pharmacokinetics. As such ML401 should be a valuable tool to explore the in vivo effects of EBI-2 inhibition.