2. Metabolic Enzyme/Protease
  3. Tryptophan Hydroxylase
  4. TPH2 agonist-1

TPH2 agonist-1 (compound 20e) 是一种口服有效、可透过血脑屏障、1,3,4-恶二唑-2 (3H)-酮衍生的 TPH2 激动剂。TPH2 agonist-1 可在 SCN1A 缺陷模型中上调 TPH2 的表达、提升 5-HT、GABA 水平，并展现出抗癫痫活性。TPH2 agonist-1 可稳定神经元网络电生理活性，抑制异常 spike 和 burst 活动。TPH2 agonist-1 无明显 hERG 抑制和细胞毒性，可用于婴儿严重肌阵挛性癫痫 (Dravet 综合征) 的相关研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

TPH2 agonist-1

TPH2 agonist-1 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

TPH2 agonist-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TPH2 agonist-1 (compound 20e) is an orally active, blood-brain barrier permeable, 1,3,4-oxadiazol-2 (3H)-one-derived TPH2 agonist. TPH2 agonist-1 upregulates TPH2 expression, elevates 5-HT and GABA levels, and exhibits antiepileptic activity in SCN1A-deficient models. TPH2 agonist-1 stabilizes the electrophysiological activity of neuronal networks and inhibits abnormal spike and burst activities. TPH2 agonist-1 shows no significant hERG inhibition or cytotoxicity, and it can be used in studies related to severe myoclonic epilepsy of infancy (Dravet syndrome)[1].

体外研究
(In Vitro)

TPH2 agonist-1 (compound 20e) 可剂量依赖性抑制 SMEI 患者来源 iPSC 神经元的异常电生理活性，1 μM 时显著降低平均放电率和爆发百分比，10 μM 和 50 μM 时进一步减少网络爆发频率和持续时间[1]。
TPH2 agonist-1 (5 μM；4 h) 处理 WT 和 scn1lab KO 斑马鱼幼虫，可升高 5 - 羟色胺 (5-HT) 和 γ- 氨基丁酸 (GABA) 水平，且能恢复 KO 幼虫下丘脑的 5-HT 免疫反应性[1]。

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

TPH2 agonist-1 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: VERO, HFL-1, L929, NIH3T3, CHO-K1
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 24 h
Result: Did not affect the viability of various mammalian cell lines, with an IC50 value greater than 100 μM in all tested cell lines as determined by WST analysis.
体内研究
(In Vivo)

TPH2 agonist-1 (compound 20e) 在小鼠模型、成年斑马鱼模型和人脑血屏障 (BBB) 系统中的脑血浆 (B/P) 比值分别为 4.36、1.75 和 0.43[1]。
TPH2 agonist-1 (5 mg/kg；灌胃给药；单次；给药后 30 min 进行热诱导) 在 SCN1A+/-小鼠中显著降低癫痫严重程度，延长首次癫痫发作潜伏期，提高发作阈值温度，且抑制小鼠过度活动，不影响野生型小鼠行为[1]。
TPH2 agonist-1 (2.5 μM、5 μM；水体暴露；单次；暴露后 30 min 记录) 在 scn1lab KO 斑马鱼幼虫中，剂量依赖性减少惊厥样运动，2.5 μM 时减少 41.58%，5 μM 时减少 16.3%，不影响野生型斑马鱼正常运动，还能恢复 KO 幼虫对蓝色的颜色偏好[1]。

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

Animal Model: 13-15-week-old male and female 129S-Scn1atm1Kea/Mmjax heterozygous mice (SCN1A+/-) and WT littermates + SMEI model[1]
Dosage: 5 mg/kg
Administration: gavage; frequency: single dose; 30 min before heat induction
Result: Significantly reduced seizure severity in SCN1A+/- mice, decreasing the Racine scale score by 52% compared with vehicle control, prolonged the latency to the first seizure, and increased the seizure threshold temperature. It also suppressed hyperactivity in SCN1A+/- mice by reducing total distance traveled and average speed, without affecting the locomotor behavior of WT mice.
分子量

373.69

Formula

C15H8ClF4N3O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TPH2 agonist-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

TPH2 agonist-1Tryptophan HydroxylaseSCN1A-deficient modelsTPH2Dravet syndrome5-HTsevere myoclonic epilepsy of infancyInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
TPH2 agonist-1
目录号：
HY-181575
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z