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• 产品描述： Phosphoramidon Disodium, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon Disodium also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively

• 靶点： Microbial Metabolite;RAAS; Neprilysin; Others

• 体外研究：
  Phosphoramidon (1-500 μM; 30 min) inhibits ET-converting enzyme (ECE) activity in a dose-dependent manner in solubilized rabbit lung membranes

• 体内研究：
  Phosphoramidon (0.25 mg/kg per min; i.v.) suppresses the hypertensive effect of big endothelin-1 in rats. Phosphoramidon (1-30 mg/kg; i.v.; once) blocks the pressor activity of porcine big endothelin-1-(1-39) in rats. Animal Model: Male Sprague-Dawley rats Dosage: 0.25 mg/kg per min Administration: Intravenous injection Result: Markedly suppressed the hypertensive effect of big endothelin-1.

• 参考文献：
  1. Umezawa S, , et al. A new microbial metabolite phosphoramidon (isolation and structure). Tetrahedron Letters, 1972, 13(1): 97-100. 2. Suda H, et al. A thermolysin inhibitor produced by actinomycetes: phosphoramidon. The Journal of antibiotics, 1973, 26(10): 621-623. 3. Kukkola PJ, et al. Differential structure-activity relationships of phosphoramidon analogues for inhibition of three metalloproteases: endothelin-converting enzyme, neutral endopeptidase, and angiotensin-converting enzyme.J CardiovascPharmacol. 1995;26Suppl 3:S65-8. 4. Matsumura Y, et al. Phosphoramidon, a metalloproteinase inhibitor, suppresses the hypertensive effect of big endothelin-1. Eur J Pharmacol. 1990 Aug 21;185(1):103-6. 5. McMahon EG, et al. Phosphoramidon blocks the pressor activity of porcine big endothelin-1-(1-39) in vivo and conversion of big endothelin-1-(1-39) to endothelin-1-(1-21) in vitro. Proc Natl Acad Sci U S A. 1991 Feb 1;88(3):703-7.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.702 ml	8.511 ml	17.022 ml
  5 mM	0.34 ml	1.702 ml	3.404 ml
  10 mM	0.17 ml	0.851 ml	1.702 ml
  50 mM	0.034 ml	0.17 ml	0.34 ml

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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 *