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(E)-3,4,5-Trimethoxycinnamic acid
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。
(E)-3,4,5-Trimethoxycinnamic acid图片
CAS NO:20329-98-0
包装与价格:
包装价格(元)
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
TMCA
产品介绍
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) 是一种被多甲氧基取代的肉桂酸。(E)-3,4,5-Trimethoxycinnamic acid 是一种口服有效的GABAA/BZ受体激动剂。(E)-3,4,5-Trimethoxycinnamic acid 与5-HT2C5-HT1A受体具有良好的结合亲和力,其IC50值分别为 2.5 和 7.6 μM。(E)-3,4,5-Trimethoxycinnamic acid 具有抗惊厥和镇静活性。(E)-3,4,5-Trimethoxycinnamic acid 可用于失眠、头痛、癫痫的研究。
生物活性

(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potentGABAA/BZreceptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to5-HT2Cand5-HT1Areceptor, withIC50values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy[1][2][3].

体外研究
(In Vitro)

(E)-3,4,5-Trimethoxycinnamic acid (10 μg/mL, 1 h) increases the expressions of GAD65and γ-subunit of GABAAreceptors in the cerebellar granule cells[3].
(E)-3,4,5-Trimethoxycinnamic acid (0-10 μg/mL, 1 h) shows a significant increase in Cl-influx[3].

Western Blot Analysis[3]

Cell Line:Primary cultured cerebellar granule cells
Concentration:10 μg/mL
Incubation Time:1 h
Result:Increased expression of GAD65(glutamic acid decarboxylase) and γ-subunit of GABAA receptors, but did not influence the amounts of a-, b-subunits in the GABAA receptors.

Cell Viability Assay[3]

Cell Line:Primary cultured cerebellar granule cells
Concentration:1, 3, 5, 10 μg/mL
Incubation Time:1 h
Result:Produced a significant increase in Cl-influx.
体内研究
(In Vivo)

(E)-3,4,5-Trimethoxycinnamic acid (0-20 mg/kg, IP, once) shows anti-seizure effects[2].
(E)-3,4,5-Trimethoxycinnamic acid (0-10 mg/kg, Orally, once) enhances hypnotic effects in pentobarbital-treated mice[3].

Animal Model:Ault male KunMing-strain mice (18-20 g, maximal electroshock (MES) and pentylenetetrazol (PTZ) models)[2]
Dosage:5, 10 and 20 mg/kg; 10 mL/kg
Administration:IP, once
Result:Significantly decreased the incidence of MES-induced THE (tonic hindlimb extension) to 50% and 20% of the value of the vehicle controls at 10 and 20 mg/kg. Decreased the incidence of MES-induced THE to only 80% at 5 mg/kg. Significantly delayed the onset of myoclonic jerks (MJ), and decreased the seizure severity and mortality compared with the vehicle-treated animals in PTZ seizure model. The incidence of generalized clonic convulsions (stage 4) disappeared at doses of both 10 and 20 mg/kg.
Animal Model:ICR male mice (25-28 g, 10-12 in each group)[3]
Dosage:2, 5 and 10 mg/kg
Administration:Orally (p.o.), once, 15 min and 1 h prior to pentobarbital injection
Result:Significantly decreased locomotor activity at 10 mg/kg. Increased NREM and total sleep, but decreased wakefulness.
Clinical Trial
分子量

238.24

性状

Solid

Formula

C12H14O5

CAS 号

20329-98-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(419.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.1974 mL20.9872 mL41.9745 mL
5 mM0.8395 mL4.1974 mL8.3949 mL
10 mM0.4197 mL2.0987 mL4.1974 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。-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 (10.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.49 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 (10.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.49 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (10.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.49 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在本网站选购。