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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Autotaxin-Autotaxin inhibitor compound 1
Autotaxin inhibitor compound 1

Chemical Structure : Autotaxin inhibitor compound 1

CAS No.: 1619971-30-0

Autotaxin inhibitor compound 1 (Autotaxin-IN-1)

货号: PC-60695Not For Human Use, Lab Use Only.

Autotaxin inhibitor compound 1 (Autotaxin-IN-1) is a potent, selective, orally bioavailable inhibitor of Autotaxin with IC50 of 2.2 nM in ex vivo human whole blood assay, does not inhibit related proteins ENPP1 and ENPP7.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Autotaxin inhibitor compound 1 (Autotaxin-IN-1) is a potent, selective, orally bioavailable inhibitor of Autotaxin with IC50 of 2.2 nM in ex vivo human whole blood assay, does not inhibit related proteins ENPP1 and ENPP7.
Autotaxin-IN-1 demonstrates significant anti-inflammatory and analgesic effects in the carrageenan-induced paw inflammation and acetic acid-induced visceral pain tests, respectively.
Autotaxin-IN-1 also significantly inhibits disease activity score in the dextran sodium sulfate-induced model of inflammatory bowel disease (IBD) and in autoimmune encephalomyelitis model of multiple sclerosis (MS).

物理化学性质&存储条件

分子量 405.462
分子式 C21H23N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-(1H-1,2,3-triazol-4-yl)ethoxy)-1-(2-((2,3-dihydro-1H-inden-2-yl)amino)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidin-6-yl)ethan-1-one

参考文献

1. Thirunavukkarasu K, et al. J Pharmacol Exp Ther. 2016 Oct;359(1):207-14.

2. Jones SB, et al. ACS Med Chem Lett. 2016 Aug 2;7(9):857-61.

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