(E)-3,4,5-Trimethoxycinnamic acid TMCA|cas:20329-98-0|西域试剂

(E)-3,4,5-Trimethoxycinnamic acid TMCA,99.95%

产品编号：Bellancom-W050162| CAS NO：20329-98-0| 分子式：C₁₂H₁₄O₅| 分子量：238.24

（E） -3,4,5-三甲氧基肉桂酸（TMCA）是一种被多甲氧基取代的肉桂酸。（E） -3,4,5-三甲氧基肉桂酸是一种口服活性强的GABAA/BZ受体激动剂。（E） -3,4,5-三甲氧基肉桂酸对5-HT2C和5-HT1A受体具有良好的结合亲和力，IC50值分别为2.5和7.6μM。（E） -3,4,5-三甲氧基肉桂酸具有抗惊厥和镇静活性。（E） -3,4,5-三甲氧基肉桂酸可用于失眠、头痛和癫痫的研究。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-W050162		￥500.00	杭州北京（现货）
Bellancom-W050162		￥800.00	杭州北京（现货）

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(E)-3,4,5-Trimethoxycinnamic acid 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-HT_2C 和 5-HT_1A 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 potent GABA_A/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT_2C and 5-HT_1A receptor, with IC₅₀ values 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.

体外研究

(E)-3,4,5-Trimethoxycinnamic acid (10 μg/mL, 1 h) increases the expressions of GAD₆₅ and γ-subunit of GABA_A receptors in the cerebellar granule cells.
(E)-3,4,5-Trimethoxycinnamic acid (0-10 μg/mL, 1 h) shows a significant increase in Cl^- influx.

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

Western Blot Analysis

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

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.
(E)-3,4,5-Trimethoxycinnamic acid (0-10 mg/kg, Orally, once) enhances hypnotic effects in pentobarbital-treated mice.

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

Animal Model:	Ault male KunMing-strain mice (18-20 g, maximal electroshock (MES) and pentylenetetrazol (PTZ) models)
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)
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.

体内研究

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

Animal Model:	Ault male KunMing-strain mice (18-20 g, maximal electroshock (MES) and pentylenetetrazol (PTZ) models)
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)
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.

体内研究

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

Animal Model:	Ault male KunMing-strain mice (18-20 g, maximal electroshock (MES) and pentylenetetrazol (PTZ) models)
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)
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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	4.1974 mL	20.9872 mL	41.9745 mL
5 mM	0.8395 mL	4.1974 mL	8.3949 mL
10 mM	0.4197 mL	2.0987 mL	4.1974 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°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 (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-CD in 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 μL 20% 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西域网站选购。

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

参考文献

. Zhao Z, et al. Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. Eur J Med Chem. 2019 Jul 1;173:213-227. [Content Brief]

. Chen CY, et al. 3,4,5-Trimethoxycinnamic acid, one of the constituents of Polygalae Radix exerts anti-seizure effects by modulating GABAAergic systems in mice. J Pharmacol Sci. 2016 May;131(1):1-5. [Content Brief]

. Lee CI, et al. 3,4,5-Trimethoxycinnamic acid (TMCA), one of the constituents of Polygalae Radix enhances pentobarbital-induced sleeping behaviors via GABAAergic systems in mice. Arch Pharm Res. 2013 Oct;36(10):1244-51. [Content Brief]

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产品编号(Item Number)

批号(Lot Number)

安全声明 (欧洲)	24/25
WGK德国	2
RTECS号	GE0722000

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(E)-3,4,5-Trimethoxycinnamic acid TMCA,99.95%

(E)-3,4,5-Trimethoxycinnamic acid TMCA

化学品安全说明书(MSDS)

质检证书(COA)

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