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• 产品描述： Sitaxsentan (sodium) is a highly selective antagonist of endothelin A receptors.

• 靶点： Endothelin Receptor

• 体内研究： Sitaxsentan和Bosentan在较高浓度下减弱NTCP转运,并抑制人肝转运蛋白,这为在临床环境中观察到的这些药物增加肝毒性提供了潜在的机制。Sitaxsentan及Sitaxsentan联合西地那非可以完全阻止内皮素-1和ETB受体的表达增加。单独使用Sitaxsentan部分恢复了BMPR-1A和BMPR-2的表达。西地那非和Sitaxsentan联用进一步恢复了BMPR-1A和BMPR-2的表达,然而,与对照相比仍然是降低的水平。

• 细胞实验： TE 671 or transfected COS 7 cells are grown to confluence in six-well plates. Sixteen hours prior to use, the media in each well is replaced with 2 mL of inositol-free RPMI-164 (IF-RPMI) media containing 10% inositol-free FCS and 2 mCi [3H]myoinositol and incubated at 37 °C in the presence of 6% CO2. The media is aspirated, and the cells are washed twice with PBS. Cells are preincubated for 10 minutes in 1 mL of lithium buffer (15 μM HEPES, pH 7.4, 145 μM NaCl, 5.4 μM KCl, 1.8 μM CaCl2, 0.8 μM MgSO4, 1.0 μM NaH2PO4, 11.2 μM glucose, 20 μM LiCl) with or without Sitaxentan sodium prior to the addition of 100 μM of ET-1 at different concentrations. Cells are then incubated for an additional 45 minutes. The buffer is discarded, and the accumulated inositol phosphates are extracted with ice cold methanol. The total cell protein in each well is measured using the BCA assay after solubilizing the cells in 0.1 M NaOH.(Only for Reference)

• 动物实验： Sitaxsentan is formulated in water.After an initial 2-week period of hypoxic exposure (10% O2) sitaxsentan (15 or 30 mg/kg body weight per day in the drinking water) is administered for 4 weeks during continuous exposure to hypoxia. At the conclusion of the 4 week period of hypoxia, femoral and pulmonary arterial cannulation and measurement of MPAP, MSAP, and HR are performed.

• 参考文献：
  1. Holm P. Scand Cardiovasc J Suppl. 1997, 46, 1-40. 2. Wu C, et al. J Med Chem. 1997, 40(11), 1690-1697. 3.Tilton RG, et al. Pulm Pharmacol Ther. 2000, 13(2), 87-97. 4.Wanebo JE, et al. Neurosurgery. 1998, 43(6), 1409-1417.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.097 ml	10.485 ml	20.969 ml
  5 mM	0.419 ml	2.097 ml	4.194 ml
  10 mM	0.21 ml	1.048 ml	2.097 ml
  50 mM	0.042 ml	0.21 ml	0.419 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 分子量 (g/mol)

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