ONX-0914 (Synonyms: PR-957)
目录号: PL10738 纯度: ≥99%
CAS No. :960374-59-8
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中文名称
ONX-0914
中文别名
ONX0914(PR-957) 抑制剂
英文名称
ONX-0914
英文别名
ONX-0914 (PR-957);(2S)-3-(4-methoxyphenyl)-N-[(2S)-1-(2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide;ONX 0914;ONX-0914;ONX0914(PR-957);PR 957;PR-957;QC-7242;N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide;N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide (ACI);L
Cas No.
960374-59-8
分子式
C31H40N4O7
分子量
580.67
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ONX-0914 (PR-957) 是选择性的低分子量多肽-7 (LMP7) 的抑制剂,LMP7 是免疫蛋白酶体的类糜蛋白酶亚单位。ONX-0914 阻断细胞因子的产生并减轻实验性关节炎的进展。ONX-0914 是分枝杆菌蛋白酶体的非竞争性不可逆抑制剂 (Ki=5.2 μM)。ONX-0914 通过 HSF-1 介导的 p-TEFb 活化激活潜伏的 HIV-1。
生物活性
ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (K i =5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
性状
Solid
IC50 & Target[1][2]
HIV-1
体外研究(In Vitro)
ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ONX-0914 (2-10 mg/kg; i.v,; on days 4, 6 and 8) meliorates disease in mouse arthritis.
ONX-0914 (2, 6 and 10 mg per kg body weight on days 25, 27, 29, 31 and 33; i.v.) treatment also induced a rapid therapeutic response in the T and B cell–dependent CIA (collagen-induced arthritis) model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis [published correction appears in Nat Med. 2009 Nov;15(11):1333]. Nat Med. 2009;15(7):781-787.
[2]. Ro?man K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020;25(6):1305. Published 2020 Mar 12.
溶解度数据
In Vitro: DMSO : ≥ 35 mg/mL (60.28 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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