1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. PNU-142633

PNU-142633 是一种高亲和力,选择性和口服活性的 5-HT1D 激动剂,对人 5-HT1D 受体和人 5-HT1B 受体的 Ki 分别为 6 nM 和 >18 000 nM。PNU-142633 具有抗偏头痛功效。

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PNU-142633 Chemical Structure

PNU-142633 Chemical Structure

CAS No. : 187665-65-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5461
In-stock
1 mg ¥2937
In-stock
5 mg ¥7343
In-stock
10 mg   询价  
50 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy[1][2].

IC50 & Target[1]

5-HT1D Receptor

6 nM (Ki)

体外研究
(In Vitro)

The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan[1].

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

体内研究
(In Vivo)

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds[1].

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

Animal Model: Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode[1]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration: Intravenous injection
Result: Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.
分子量

422.52

Formula

C24H30N4O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 42 mg/mL (99.40 mM; 超声加热助溶; 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 2.3668 mL 11.8338 mL 23.6675 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 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。-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

纯度: ≥98.0%

参考文献

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。-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 2.3668 mL 11.8338 mL 23.6675 mL 59.1688 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL 11.8338 mL
10 mM 0.2367 mL 1.1834 mL 2.3668 mL 5.9169 mL
15 mM 0.1578 mL 0.7889 mL 1.5778 mL 3.9446 mL
20 mM 0.1183 mL 0.5917 mL 1.1834 mL 2.9584 mL
25 mM 0.0947 mL 0.4734 mL 0.9467 mL 2.3668 mL
30 mM 0.0789 mL 0.3945 mL 0.7889 mL 1.9723 mL
40 mM 0.0592 mL 0.2958 mL 0.5917 mL 1.4792 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1834 mL
60 mM 0.0394 mL 0.1972 mL 0.3945 mL 0.9861 mL
80 mM 0.0296 mL 0.1479 mL 0.2958 mL 0.7396 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:
PNU-142633
目录号:
HY-103131
需求量: