货号	规格	价格	上海	北京	武汉	南京
S85015-5mg	≥98%	￥1100.00 S85015-5mg ￥1100.00 2-3天	0 货期：2-3天	-	-	-
S85015-10mg	≥98%	￥1800.00 S85015-10mg ￥1800.00 2-3天	0 货期：2-3天	-	-	-
S85015-50mg	≥98%	￥7500.00 S85015-50mg ￥7500.00 2-3天	0 货期：2-3天	-	-	-

货号

规格

价格

上海

北京

武汉

南京

购买数量

S85015-5mg

≥98%

￥1100.00

货期：2-3天

S85015-10mg

≥98%

￥1800.00

货期：2-3天

S85015-50mg

≥98%

￥7500.00

货期：2-3天

产品介绍

产品描述：

靶点：

EC50: 3 nM (GABAA α5) Ki: 0.83 nM (Human GABAA α1β3γ2), 0.85 nM (Human GABAA α2β3γ2), 0.77 nM (Human GABAA α3β3γ2), 1.4 nM (Human GABAA α5β3γ2)

体外研究：

MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively. MRK-016 is a full inverse agonist at the α5-subtype, shows very weak affinity at the GABAA α4β3γ2-subtype (Ki 395 ± 173 nM) and is essentially inactive at the GABAA α6β3γ2 receptor (Ki > 4000 nM). MRK-016 shows a weak effect on GABAA α4β3γ2 with a Ki of 400 nM. MRK-016 (100 nM) alao increases long-term potentiation in mouse hippocampal slices

体内研究：

MRK-016 does not enhance pentylenetetrazole-induced convulsions at 10 mg/kg via ip, or cause seizures at 30 mg/kg, via po for 20 days in mice. MRK-016 shows no obvious anxiogenic-like effects in rats at doses that occupy >95% of benzodiazepine (BZ) binding sites. MRK-016 (0.3, 1, and 3 mg/kg, p.o.) dose-dependently improves performance of rats hippocampal-dependent memory task. MRK-016 (0.3-30 mg/kg, p.o.) causes good receptor occupancy in rats. MRK-016 (0.3, 1, or 3 mg/kg p.o.) shows cognition-enhancing activity in the delayed matching-to-position version of the Morris water maze. MRK-016 (1, 3, or 10 mg/kg i.p.) does not produce kindling in mice. MRK-016 (3 mg/kg, i.p.) protects against LPS-induced learning/memory decrements in mice

参考文献：

1. Chambers MS, et al. An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. J Med Chem. 2004 Nov 18;47(24):5829-32. 2. Atack JR, et al. In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. 3. Eimerbrink MJ, et al. Administration of the inverse benzodiazepine agonist MRK-016 rescues acquisition and memory consolidation following peripheral administration of bacterial endotoxin. Behav Brain Res. 2015 Jul 15;288:50-3.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.714 ml	13.572 ml	27.145 ml
5 mM	0.543 ml	2.714 ml	5.429 ml
10 mM	0.271 ml	1.357 ml	2.714 ml
50 mM	0.054 ml	0.271 ml	0.543 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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