1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. NAS-181 dimesylate

NAS-181 dimesylate 

目录号: HY-103156 纯度: 98.44%
COA 产品使用指南

NAS181 是一种有效和选择性的大鼠 5-HT1B 受体拮抗剂,Ki 值为 47 nM。NAS181 对 r5-HT1B 的选择性比牛 5-HT1B 受体 (Ki=630 nM) 高 13 倍。NAS181 通过抑制末端 r5-HT1B 自身受体来增加 5-HT 转换和 5-HT 的突触浓度。

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NAS-181 dimesylate Chemical Structure

NAS-181 dimesylate Chemical Structure

CAS No. : 1217474-40-2

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1 mg ¥1272
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5 mg ¥2800
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10 mg ¥4500
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25 mg ¥9000
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Customer Review

Other Forms of NAS-181 dimesylate:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors[1][2].

IC50 & Target[1]

Rat 5-HT1B Receptor

47 nM (IC50)

体外研究
(In Vitro)

NAS181 has very low affinities (Ki>3000 nM) for all other receptors examined, including 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7, α1-, α2-, and β-adrenoceptors, and dopamine D1 and D2[1].
NAS181 (10-1000 nM) dose-dependently potentiates the K+-stimulated [3H]-5-HT release in preloaded rat occipital cortical slices[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NAS181 (1-10 mg/kg; s.c.) dose-dependently increases acetylcholine (ACh) release in the frontal, ventral hippocampus cortex and VHipp[1].
NAS181 (20 mg/kg; s.c.) enhances the 5-HT turnover in four rat brain regions (hypothalamus, hippocampus, striatum, and frontal cortex) with about 40%[1].
NAS181 (3 mg/kg; s.c.) produces a significant increase in the number of wet dog shakes in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male Sprague-Dawley rats (250-300 g)
Dosage: 1, 5, 10 mg/kg
Administration: S.c. in the scruff of the neck
Result: Increased the ACh release in the frontal cortex, reaching the maximal value of 500% of the control group within 80 min after the injection of the highest dose.
Increased the ACh releases in VHipp with a maximum of 230% of the control values at 80 min after the injection of the highest dose.
分子量

538.63

Formula

C21H34N2O10S2

CAS 号
非同位 CAS

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 62.5 mg/mL (116.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8566 mL 9.2828 mL 18.5656 mL
5 mM 0.3713 mL 1.8566 mL 3.7131 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

NAS-181 dimesylate 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8566 mL 9.2828 mL 18.5656 mL 46.4141 mL
5 mM 0.3713 mL 1.8566 mL 3.7131 mL 9.2828 mL
10 mM 0.1857 mL 0.9283 mL 1.8566 mL 4.6414 mL
15 mM 0.1238 mL 0.6189 mL 1.2377 mL 3.0943 mL
20 mM 0.0928 mL 0.4641 mL 0.9283 mL 2.3207 mL
25 mM 0.0743 mL 0.3713 mL 0.7426 mL 1.8566 mL
30 mM 0.0619 mL 0.3094 mL 0.6189 mL 1.5471 mL
40 mM 0.0464 mL 0.2321 mL 0.4641 mL 1.1604 mL
50 mM 0.0371 mL 0.1857 mL 0.3713 mL 0.9283 mL
60 mM 0.0309 mL 0.1547 mL 0.3094 mL 0.7736 mL
80 mM 0.0232 mL 0.1160 mL 0.2321 mL 0.5802 mL
100 mM 0.0186 mL 0.0928 mL 0.1857 mL 0.4641 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NAS-181 dimesylate
目录号:
HY-103156
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