DO-264

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

DO-264 是一个具有体内活性的、自水解酶结构域 12(ABHD12) 的抑制剂，其 IC50 值为 11 nM。

DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.

DO-264 displays an IC50 value of 11 nM (9.6 nM-13 nM). DO-264 blocks lyso-PS hydrolysis activities of recombinant mouse and human ABHD12 in transfected HEK293T cell lysates (DO-264 IC50 values of ~30 and 90 nM against mouse and human ABHD12, respectively) and the ABHD12-dependent lyso-PS lipase activity of membrane lysates from mouse brain (IC50=2.8 nM, 2.4 nM-3.3 nM) and human THP-1 cells (IC50= 8.6 nM, 6.3 nM-12 nM).

Mice treated with DO-264 display dose-dependent increases in brain lyso-PS and 20:4 PS content that are qualitatively similar to the changes observed in ABHD12–/– mice. DO-264-treated mice, however, show minimal impairment in auditory function following four weeks of drug exposure. Both ABHD12–/– and DO-264-treated mice display exacerbated immunopathology following infection with the lymphocytic choriomeningitis virus (LCMV) clone 13, resulting in severe inflammatory lung damage, heightened chemokine production, and, in some cases, death.

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Others

Other Targets

Others

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2301866-59-9

558.4

C23H20Cl2F3N5O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 100 mg/mL (179.08 mM )

FC(F)(F)Oc1ccc(Oc2ccnc(N3CCC(CC3)NC(=S)Nc3cccnc3)c2Cl)c(Cl)c1

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(-20℃)

With Ice Pack

≥ 2 years