HA130

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Chemical Structure| 1229652-21-4 同义名 : -
CAS号 : 1229652-21-4
货号 : A662242
分子式 : C24H19BFNO5S
纯度 : 99%
分子量 : 463.29
MDL号 : MFCD20926343
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(86.34 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Autotaxin (ATX) is an ectoenzyme that catalyzes the conversion of lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), a bioactive lipid and a close relative of sphingosine 1-phosphate. High endothelial venules (HEVs) produce and secrete ATX into the blood[3]. HA130 is a selective ATX inhibitor with an IC50 of 28 nM[3]. HA130 abolished the enhancing effect of ATX on TEM (transendothelial migration) and HA130 at 0.3 mM completely ablated the activity of ATX on TK1 uropod formation[3]. When injecting CFSE-labeled T cells together with HA130 i.v. into mice and then reinjecting the drug at 7 and 12 min, SLOs (secondary lymphoid organs) were sectioned and stained to reveal HEVs after 15 min[3]. The ratio of outside HEVs to inside HEVs was used as an index of T cell migration across HEVs. HA130 decreased the outside HEV/inside HEV ratio by 3–4-fold compared with vehicle treatment (p＜0.01 for both PLNs (peripheral lymph node) and MLNs (mesenteric lymph node)). This result is consistent with HA130 retarding the migration of T cells across LN (lymph node) HEVs[3]. The s.c. administration of HA130 induces marked lymphocyte accumulation within the endothelial cell (EC) and sub-EC layers of HEVs in draining lymph nodes[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.58mL

4.32mL

2.16mL
参考文献

[1]Albers HM, van Meeteren LA, et al. Discovery and optimization of boronic acid based inhibitors of autotaxin. J Med Chem. 2010 Jul 8;53(13):4958-67.

[2]Albers HM, Dong A, et al. Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation. Proc Natl Acad Sci U S A. 2010 Apr 20;107(16):7257-62.

[3]Zhang Y, Chen YC, Krummel MF, Rosen SD. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J Immunol. 2012 Oct 15;189(8):3914-24. doi: 10.4049/jimmunol.1201604. Epub 2012 Sep 7. PMID: 22962684; PMCID: PMC3509168.

[4]Bai Z, Cai L, Umemoto E, Takeda A, Tohya K, Komai Y, Veeraveedu PT, Hata E, Sugiura Y, Kubo A, Suematsu M, Hayasaka H, Okudaira S, Aoki J, Tanaka T, Albers HM, Ovaa H, Miyasaka M. Constitutive lymphocyte transmigration across the basal lamina of high endothelial venules is regulated by the autotaxin/lysophosphatidic acid axis. J Immunol. 2013 Mar 1;190(5):2036-48. doi: 10.4049/jimmunol.1202025. Epub 2013 Jan 30. PMID: 23365076.