您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Frovatriptan succinate hydrate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Frovatriptan succinate hydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Frovatriptan succinate hydrate图片
CAS NO:158930-17-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
(R)-Frovatriptan succinate hydrate
SB 209509 succinate hydrate
VML 251 succinate hydrate
产品介绍
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) 是一种强效,高亲和力,选择性和具有口服活性的5-HT1B(pK50为 8.2) 和5-HT1D受体激动剂,选择性是 5-HT1A,5-HT1F和 5-HT7的 10 倍以上,是其他 5-HT,多巴胺,组胺 H1和 α1-肾上腺素受体的 1000 倍以上。Frovatriptan succinate hydrate 可用于偏头痛的研究。
生物活性

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active5-HT1B(pK50of 8.2) and5-HT1Dreceptoragonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for5-HT1Band5-HT1Dover 5-HT1A, 5-HT1F, and 5-HT7and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research[1][2].

IC50& Target

5-HT1BReceptor

8.2 (pEC50)

5-HT1DReceptor

 

体外研究
(In Vitro)

Cerebral vasodilatation and neurogenic inflammation are considered to be prime movers in the pathogenesis of migraine. Activation of 5-HT1Breverses cerebral vasodilatation and activation of 5-HT1Dprevents neurogenic inflammation. Frovatriptan has a high affinity for 5-HT1Band 5-HT1Dreceptors and a moderate affinity for the 5-HT1Aand 5-HT1Freceptors subtypes. Frovatriptan has a moderate affinity for the 5-HT7receptors, an action associated with coronary artery relaxation in the dog[1].

体内研究
(In Vivo)

Oral bioavailability of Frovatriptan is 22%-30% and is not affected by food. Although the maximum concentration in the plasma is achieved in 2-3 hours, 60%-70% of this is achieved in 1 hour. A steady state is achieved in 4-5 days. Plasma protein binding is low at 15%. The most unique feature is the relative terminal long half-life of about 26 hours. Frovatriptan is chiefly metabolized by CYP1A2 and is cleared by the kidney and liver making moderate failure of either organ not a limiting factor in treatment[1].
Frovatriptan (0.1, 0.2, and 0.3 mg/kg; a single bolus intraduodenal administration) treatment produces an increase in carotid vascular resistance, which is sustained for at least 5 hours in dogs[2].

Clinical Trial
分子量

379.41

性状

Solid

Formula

C18H25N3O6

CAS 号

158930-17-7

中文名称

夫罗曲坦琥珀酸盐水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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
In Vitro: 

DMSO : 100 mg/mL(263.57 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6357 mL13.1784 mL26.3567 mL
5 mM0.5271 mL2.6357 mL5.2713 mL
10 mM0.2636 mL1.3178 mL2.6357 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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 (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。