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• 产品描述： S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization

• 靶点： Sigma 1 Receptor;Sigmareceptor

• 体外研究：
  S1RA hydrochloride (0.1-10000 nM) 对人和豚鼠的 σ1R 的 Ki 值分别为 17 和 23.5 nM。 S1RA hydrochloride (0.1-10000 nM) 对人 σ2R 具有亲和力，Ki 值为 9.3 μM。 S1RA hydrochloride 对人 5-HT2B 受体具有亲和力，Ki 值为 328 nM，IC50 值为 4.7 μM

• 体内研究：
  S1RA hydrochloride (腹腔注射 16-80 mg/kg 或口服 32-128 mg/kg；一次) 剂量依赖性地抑制小鼠中福尔马林诱导的痛觉，辣椒素诱导的机械超敏反应和坐骨神经损伤诱导的机械和热超敏反应。 Animal Model: Male CD1 mice Dosage: 32, 64, 128 and 160 mg/kg Administration: Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once Result: Reduced the permanence time on the rotating rod in rotarod test. Animal Model: Male CD1 mice with formalin-evoked nociception Dosage: 20, 40 and 80 mg/kg Administration: Intraperitoneal injection; 20, 40 and 80 mg/kg, once Result: Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice. Animal Model: Male CD1 mice with capsaicin-induced mechanical hypersensitivity Dosage: 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration) Administration: Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once Result: Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.

• 参考文献：
  1. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306. 2. Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.675 ml	13.373 ml	26.747 ml
  5 mM	0.535 ml	2.675 ml	5.349 ml
  10 mM	0.267 ml	1.337 ml	2.675 ml
  50 mM	0.053 ml	0.267 ml	0.535 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 *