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• 产品描述： SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM)

• 靶点： 5-HT6 Receptor:8.92-9.02 (pKi);5-HT1D Receptor:6.55 (pKi);5-HT1A Receptor:6.35 (pKi);5-HT1B Receptor;6.05 (pKi);5-HT1F Receptor:5.95 (pKi);5-HT2A Receptor:5.62 (pKi);5-HT2B Receptor:5.41 (pKi);5-HT7 Receptor:5.39 (pKi);5-HT4 Receptor:5.27 (pKi);5-HT1E Receptor:<4.99 (pKi);Human 5-HT2C Receptor:5.73 (pKi);5-HTReceptor

• 体外研究：
  SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71

• 体内研究：
  SB 271046 Hydrochloride (10 mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg/kg p.o. and maximum effect at 4 h post-dose Animal Model: Male Sprague Dawley rats Dosage: 10 mg/kg Administration: P.o. Result: Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg kg−1 p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax.

• 参考文献：
  1. Routledge C, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000;130(7):1606-1612.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： 2-8℃;干燥

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.047 ml	10.236 ml	20.473 ml
  5 mM	0.409 ml	2.047 ml	4.095 ml
  10 mM	0.205 ml	1.024 ml	2.047 ml
  50 mM	0.041 ml	0.205 ml	0.409 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 *