• 產(chǎn)品描述： UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM

• 靶點(diǎn)： IC50: 0.48 nM (DPPII); Ki: 0.082 nM (DPPII);Proteasome

• 體外研究：
  UAMC00039 has an IC50 of 0.48±0.04 nM and a high selectivity for DPPII compared to DPPIV (IC50=165±9 μM) and DPP activity not caused by DPPII or DPPIV. UAMC00039 seems a promising tool to unravel the function of DPPII as well as to validate its potential as a therapeutic target. The efficacy of a DPPII inhibitor in cell culture depends not only on the inhibitors’ potency towards the enzyme but also on its stability in the medium and its ability to enter the cell. UAMC00039 is stable for at least 48 h at 37 °C in culture medium and in DPPII assay buffer. The compound is able to enter PBMC within 1 min resulting in a concentration-dependent inhibition of intracellular DPPII activity without affecting the ‘non-DPPII’ DPP activity. 1 and 100 μM UAMC00039 inhibits DPPII activity of PBMC and U937 cells more than 90%

• 體內(nèi)研究：
  A dose dependent inhibition of DPPII but not of DPPIV is observed in the peripheral organs of both the rats and the mice (after oral administration) and the rabbits (after IV administration). UAMC00039 tested orally at 2 mg/kg does not cause signs of acute toxicity and does not cause any significant changes in the following functions that are evaluated: general behaviour, body temperature, respiration, bleeding time, blood pressure, urine volume, liver function, fasting glucose and gastrointestinal parameters like acidity, motility and irritation

• 參考文獻(xiàn)：
  1. Maes MB, et al. In vivo effects of a potent, selective DPPII inhibitor: UAMC00039 is a possible tool for the elucidation of the physiological function of DPPII. Adv Exp Med Biol. 2006;575:73-85. 2. Maes MB, et al. Dipeptidyl peptidase II and leukocyte cell death. Biochem Pharmacol. 2006 Jun 28;72(1):70-9.

• 溶解性： Soluble  in  DMSO、H2O

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.613 ml	13.063 ml	26.126 ml
  5 mM	0.523 ml	2.613 ml	5.225 ml
  10 mM	0.261 ml	1.306 ml	2.613 ml
  50 mM	0.052 ml	0.261 ml	0.523 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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