Autotaxin inhibitor compound 1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Autotaxin抑制剂化合物1 (Autotaxin-IN-1)是一种有效的、选择性的、口服生物可利用的autotaxin抑制剂，在离体人全血测定中IC50为2.2 nM。

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; demonstrates significant anti-inflammatory and analgesic effects in the carrageenan-induced paw inflammation and acetic acid-induced visceral pain tests, respectively; 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).

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Autotaxin-IN-1 (i.v.; 1.0mg/kg) has T1/2 of 1.14 hours.Autotaxin-IN-1 (p.o.; 10 mg/kg) has Cmax of 660 nM and AUC of 3440 nM?h. Animal Model:Normal ratDosage:1.0 mg/kg, 10 mg/kg (Pharmacokinetic Study) Administration:I.v. (1.0 mg/kg); p.o. (10 mg/kg)Result:Has T1/2 of 1.14 hours (i.v.; 1.0mg/kg).Has Cmax of 660 nM and AUC of 3440 nM?h (p.o.; 10 mg/kg).

Autotaxin-IN-1

Wnt/Notch/Hedgehog

Autotaxin

Autotaxin

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1619971-30-0

405.462

C21H23N7O2

>98% (HPLC)

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O=C(N1CC2=NC(NC3CC4=C(C=CC=C4)C3)=NC=C2C1)COCCC5=CNN=N5

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

(-20℃)

With Ice Pack

≥ 2 years