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• 产品描述： Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders

• 靶点： IC50: 8 nM (GABAAα5) Ki: 5 nM (GABAAα5); 1031 nM (GABAAα1); 458 nM (GABAAα2); 510 nM (GABAAα3);GABAReceptor

• 体外研究：
  Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors. Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM. Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes

• 体内研究：
  Basmisanil (3-100 mg/kg, p.o.) occupies GABAA-α receptor in dose-dependent in rat brain. Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects. Animal Model: Sprague Dawley rats(180 g; female) Dosage: 3-100 mg/kg Administration: p.o. Result: Decreased the binding of [3H]-Ro 15-4513 in a dose-dependent manner.Reduced specific binding in the hippocampus by 70% at the highest dose (100 mg/kg). Animal Model: Lister Hooded rats, Wistar rats and F-344 Fischer rats(Lister Hooded rats: 220-250 g; male)(Wistar rats: 200-220 g; male and female)(F-344 Fischer rats: 170-180 g; male) Dosage: 3-600 mg/kg Administration: p.o. Result: Significantly attenuated the diazepam-induced deficit.Showed plasma concentrations in dose- and time-dependent manner and reached a maximal level of 903 ng/mL (379 nM free plasma) 30 min after the administration at 10 mg/kg. Animal Model: Male cynomolgus macaques(Macaca fascicularis; 7-10 kg) Dosage: 1-600 mg/kg Administration: p.o. Result: Significantly improved the percentage of correct first reaches during difficult trials of the object retrieval task at the 3 and 10 mg/kg doses.Exhibited an inverted U-shaped dose response in this paradigm with the 1 and 30 mg/kg doses producing no marked improvement on performance.Increased the total plasma exposure in dose-dependent.

• 参考文献：
  1. Joerg F Hipp, et al. Basmisanil, a highly selective GABA A-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. Sci Rep. 2021 Apr 8;11(1):7700.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.245 ml	11.224 ml	22.449 ml
  5 mM	0.449 ml	2.245 ml	4.49 ml
  10 mM	0.224 ml	1.122 ml	2.245 ml
  50 mM	0.045 ml	0.224 ml	0.449 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 *