货号	规格	价格	上海	北京	珠海	重庆	武汉
S86663-5mg促销	≥98%	￥150.00 ￥135.00 S86663-5mg ￥135.00 现货	9 0 9	-	-	-	-
S86663-10mg促销	≥98%	￥260.00 ￥234.00 S86663-10mg ￥234.00 现货	7 7	-	-	-	-
S86663-25mg促销	≥98%	￥500.00 ￥450.00 S86663-25mg ￥450.00 现货	5 5	-	-	-	-
S86663-50mg促销	≥98%	￥870.00 ￥782.00 S86663-50mg ￥782.00 现货	1 1	-	-	-	-
S86663-100mg促销	≥98%	￥1400.00 ￥1260.00 S86663-100mg ￥1260.00 现货	2 2	-	-	-	-

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产品描述：

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively

靶点：

5-HT2A Receptor:1.7 nM (IC50);5-HT2C Receptor:79 nM (IC50);5-HT2B Receptor:791 nM (IC50);5-HTReceptor

体内研究：

Each compound is tested in a minimum of five rats by oral gavage with administration occurring in the middle of the inactive period, 6 h after light onset. The delta power during non-REM sleep (NREMS) is significantly different between all the analogues tested and the vehicle control. Nelotanserin (Compound 39) produces significant increases in delta power that persist for the first 4 h following dosing. Significant differences are found, however, in NREMS bout length. Nelotanserin significantly increases NREMS bout length during the first hour following dosing, and 3 does so during the second hour. In conjunction with this increased NREM bout duration, the number of NREM bouts decrease during the first hour for Nelotanserin (p<0.01) as well as for compound 15 (p<0.05)

参考文献：

1. Al-Shamma HA et al. Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia. J Pharmacol Exp Ther. 2010 Jan;332(1):281-90. 2. Teegarden BR et al. Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia. J Med Chem. 2010 Mar 11;53(5):1923-36.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.287 ml	11.435 ml	22.871 ml
5 mM	0.457 ml	2.287 ml	4.574 ml
10 mM	0.229 ml	1.144 ml	2.287 ml
50 mM	0.046 ml	0.229 ml	0.457 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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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

Nelotanserin (APD125)

1-[3-(4-Bromo-1-methyl-1H-pyrazol-5-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)