Zolmitriptan - CAS:139264-17-8

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Zolmitriptan (Synonyms:BW-311C90; 311C90)

目录号 : KM12730 CAS No. : 139264-17-8 纯度 : 98%

Data Sheet 产品使用指南

Zolmitriptan (BW-311C90; 311C90) 是一种 5-HT1B/1D 受体部分激动剂，对 5-HT1B、5-HT1D、5-HT1F 受体的 K_i 分别为 5.01 nM、0.63 nM 和 63.09 nM。Zolmitriptan可用于偏头痛的研究。

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500mg		In-stock
1g	询价	In-stock
5g	询价	In-stock

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生物活性

Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine.

体外研究

Zolmitriptan (311C90) exhibits higher affinity to 5-HT than sumatriptan (pK_A=6.63±0.04 and 6.16±0.03, respectively). 311C90 displays high affinity at human recombinant 5-HT1D and 5-HT1B receptors in transfected CHO-K1 cell membranes (pIC₅₀ values=9.16±0.12 and 8.32±0.09, respectively) .

体内研究

"Zolmitriptan (311C90; 3-30 μg/kg, i.v.) causes a dose-dependent inhibition of [I]-albumin extravasation within the ipsilateral dura mater. Zolmitriptan also produces dose-dependent falls in cranial vascular conductance (32.3% at 30 μg/kg). Zolmitriptan is an anti-migraine agent with action at 5-HT1B/D receptors. Zolmitriptan is an effective and behaviorally specific anti-aggressive agent in situations that engender moderate and alcohol-heightened levels of aggression. Zolmitriptan (1-30 mg/kg, i.p.) exerts behaviorally specific anti-aggressive effects in mice."

Animal Model:	Anaesthetized guinea-pigs
Dosage:	0, 3, 10, 30 μg/kg
Administration:	I.v.
Result:	In vehicle-treated animals, unilateral electrical stimulation of the trigeminal ganglion increased extravasation of [125I]-albumin into the dura on the side ipsilateral to stimulation producing a stimulated/unstimulated ratio of 1.57. Zolmitriptan decreased this ratio in a dose-dependent fashion. Zolmitriptan produced concomitant, dose-related falls in ear conductance.

Animal Model:	Adult male CFW mice weighing approximately 25 g
Dosage:	1, 3, 5.6, 10, 30, 56 mg/kg
Administration:	Administered i.p. in a volume of 1 mL/100 g body weight
Result:	Significantly decreased the frequency of attack bites.

分子式

C₁₆H₂₁N₃O₂

分子量

287.36

CAS号

139264-17-8

中文名称

佐米曲普坦

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 : 100 mg/mL (348.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4800 mL	17.3998 mL	34.7996 mL
5 mM	0.6960 mL	3.4800 mL	6.9599 mL
10 mM	0.3480 mL	1.7400 mL	3.4800 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: 2.5 mg/mL (8.70 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。