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• 产品描述： 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 (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1

• 靶点： HIV-1;Proteasome; HIVProtease; Antibacterial

• 体外研究：
  ONX-0914 抑制 LMP7 特异性抗原呈递。ONX-0914 阻断小鼠脾细胞产生细胞因子并阻断 T 细胞分化

• 体内研究：
  ONX-0914 (2-10 mg/kg；静脉注射；在第 4、6 和 8 天) 改善小鼠关节炎的疾病。 ONX-0914 (第 2、6 和在第 25、27、29、31 和 33 天，每公斤体重 10 毫克；iv) 处理还在 T 和 B 细胞依赖性 CIA (胶原诱导的关节炎) 模型中诱导了快速处理反应。 Animal Model: Collagen antibody-induced arthritis (CAIA, Arthritis was induced in BALB/c mice with antibodies specific for type II collagen (mAb) and endotoxin) Dosage: 2, 6 or 10 mg per kg body weight Administration: I.v.; treated on days 4, 6 and 8 Result: Blocked disease progression in a dose-dependent manner and completely ameliorated visible signs of disease at the highest dose.

• 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. Rožman K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020;25(6):1305. Published 2020 Mar 12. 3. Lin J, et al. PR-957, a selective immunoproteasome inhibitor, reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1. Biochem Pharmacol. 2018;156:511-523.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.722 ml	8.611 ml	17.221 ml
  5 mM	0.344 ml	1.722 ml	3.444 ml
  10 mM	0.172 ml	0.861 ml	1.722 ml
  50 mM	0.034 ml	0.172 ml	0.344 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *