货号	规格	价格	上海	北京	珠海	重庆	武汉
S89665-5mg买3赠1	≥98%	￥2040.00 S89665-5mg ￥2040.00 现货（买3赠1）	100 >10	-	-	-	-
S89665-10mg买3赠1	≥98%	￥2890.00 S89665-10mg ￥2890.00 现货（买3赠1）	50 >10	-	-	-	-
S89665-25mg	≥98%	￥5090.00 S89665-25mg ￥5090.00 现货	20 >10	-	-	-	-
S89665-100mg	≥98%	￥9990.00 S89665-100mg ￥9990.00 现货	5 5	-	-	-	-

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产品描述：

Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders

靶点：

Histamine Receptor;HistamineReceptor

体外研究：

Samelisant free base displays inverse agonist activity and it exhibits very high selectivity towards H3R. The pEC50 value of histamine (8.5) for human H3 receptor increases to 8.2, 7.3 and 6.2 after treatment with 1, 10 and 100 nM of Samelisant, respectively. The pEC50 value of histamine (8.2) for rat H3 receptor increases to 7.9, 7.4 and 6.4 after treatment with 1, 10 and 100 nmol/L of Samelisant, respectively.
Samelisant free base binds to the orthosteric site in a reversible manner with Kb values of 1.3 nM and 1.1 nM deduced from pA2 value for human and rat H3R, respectively.
Samelisant free base also modulates dopamine and norepinephrine levels in the cerebral cortex while it has no effects on dopamine levels in the striatum or nucleus accumbens.

体内研究：

Treatment with Samelisant (10 and 30 mg/kg, p.o.) produces a significant increase in wakefulness with a concomitant decrease in non-rapid eye movement sleep (NREM) sleep in orexin knockout mice subjected to sleep electroencephalography (EEG). Samelisant also produces a significant decrease in direct rapid eye movement (REM) sleep onset (DREM) episodes, demonstrating its anticataplectic effects in an animal model relevant to narcolepsy. Samelisant treatment in mice produces a dose-dependent increase in tele-methylhistamine levels indicating the activation of histaminergic neurotransmission. Animal Model: Male Wistar rats or male C57BL6J mice Dosage: 1, 3, 10, and 30 mg/kg Administration: Oral administration Result: Produced a dose-dependent increase in t-MH levels in the frontal cortex, hypothalamus and cerebrospinal fluid (CSF) of male Wistar rats. Produced a significant increase in t-MH levels of the frontal cortex, striatum and hypothalamus in mice.

参考文献：

1. Ramakrishna Nirogi, et al. Samelisant (SUVN-G3031), a potent, selective and orally active histamine H3 receptor inverse agonist for the potential treatment of narcolepsy: pharmacological and neurochemical characterisation. Psychopharmacology (Berl). 2021 Jun;238(6):1495-1511.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.677 ml	13.387 ml	26.774 ml
5 mM	0.535 ml	2.677 ml	5.355 ml
10 mM	0.268 ml	1.339 ml	2.677 ml
50 mM	0.054 ml	0.268 ml	0.535 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

SUVN-G3031

N-[4-(1-cyclobutyl piperidin-4-yloxy)-phenyl]-2-(morpholin-4-yl) acet amide

参考文献

质检证书(COA)

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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)