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• 产品描述： Olodanrigan (EMA401, PD-126055, (S) PD-126055) 是一种高度选择性的、具有口服活性的外周限制性 angiotensin II type 2 receptor (AT2R) 拮抗剂。Olodanrigan 的镇痛作用可能涉及抑制增强 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活，从而抑制 DRG 神经元过度兴奋和 DRG 神经元的萌芽

• 靶点： AT2R;RAAS

• 体外研究：
  EMA401 may act on paracrine/autocrine mechanisms at peripheral nerve terminals, or intracrine mechanisms, to reduce neuropathic pain signalling in AngII/NGF/TRPV1-convergent pathways

• 体内研究：
  EMA401, a selective small molecule antagonist of the AT2R, results in a significant attenuation of theta power and increase in paw withdrawal latencies (PWL) in rats at day 14 after chronic constriction injury (CCI).

• 细胞实验： Cell lines: rat DRG neurons Concentrations: 10, 100 nM Incubation Time: 30 min Method: 48 h after plating, duplicate dishes were treated with AngII (10 nM), AngII + EMA401 (10 and 100 nM respectively), 100 nM EMA401, NGF (100 ng/ml) or vehicle treated (control 0), for 30 min at 37 ℃, then fixed with 4% PFA for 30 min for immunostaining.

• 动物实验： Animal Models: Adult male Sprague-Dawley (SD) rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve Dosages: 1 mg/kg (i.v.); 10 mg/kg (p.o.) Administration: i.v.; p.o.

• 参考文献：
  1. Anand U, et al. Mechanisms underlying clinical efficacy of Angiotensin II type 2 receptor (AT2R) antagonist EMA401 in neuropathic pain: clinical tissue and in vitro studies. Mol Pain. 2015 Jun 26;11:38. 2. Smith MT, et al.Small molecule angiotensin II type 2 receptor (AT₂R) antagonists as novel analgesics for neuropathic pain: comparative pharmacokinetics, radioligand binding, and efficacy in rats. Pain Med. 2013 May;14(5):692-705.

• 溶解性： DMSO:  ≥  34  mg/mL

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.97 ml	9.851 ml	19.701 ml
  5 mM	0.394 ml	1.97 ml	3.94 ml
  10 mM	0.197 ml	0.985 ml	1.97 ml
  50 mM	0.039 ml	0.197 ml	0.394 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 *