1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Trap-101 hydrochloride

Trap-101 hydrochloride 

目录号: HY-11052A
产品使用指南

Trap-101 hydrochloride 是一种有效的,选择性和竞争性的 NOP receptors 拮抗剂 ,对 NOP 受体的选择性高于对其他的阿片受体。Trap-101 刺激 GTPγ35S 结合到 CHOhNOP,NOP、μ-,κ- 和 δ 阿片受体的 pKi 值分别为 8.65, 6.60, 6.14 和 <5。Trap-101 减弱帕金森病大鼠运动缺陷,可用于神经系统疾病的研究。

MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务

Trap-101 hydrochloride Chemical Structure

Trap-101 hydrochloride Chemical Structure

CAS No. : 1216621-00-9

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

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

Description

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases[1].

IC50 & Target

pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5 (δ-opioid receptor)[1]

In Vitro

Trap-101 hydrochloride (3, 30, and 300 nM) is inactive per se up to 10 μM, while in the range 3-300 nM, it produces a concentration dependent rightward shift of the concentration-response curve to N/OFQ without modifications of the maximal response to the agonist. Receptor binding affinities of Trap101 (pKi values) at recombinant human NOP, and classical opioid receptors expressed in CHO cell membranes are 8.65, 6.60, 6.14 and < 5 for NOP, μ-, κ-, and δ-opioid receptors respectively[1].

In Vivo

Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in naïve rats, it causes a delayed increase in the immobility time in the bar test at 30 mg/kg, Moreover, it increased stepping activity and rotarod performance at 10 mg/kg and reduces them at 30 mg/kg[1].
6-OHDA lesioning produces motor asymmetry mostly affecting the contralateral paw and overall reduced motor performance. Trap-101 hydrochloride (intraperitoneal injection; 10-30 mg/kg; detected after 90 min) alleviates akinesia/bradykinesia and improves overall gait ability in hemiparkinsonian rats, being effective starting at 1 mg/kg and without worsening motor deficit at 30 mg/kg[1].

Animal Model: 6-OHDA hemilesioned rats[1]
Dosage: 10-30 mg/kg
Administration: Intraperitoneal injection; 10-30 mg/kg; detected after 90 min
Result: Attenuated parkinsonian-like motor deficits in rat.
Molecular Weight

434.01

Formula

C₂₄H₃₆ClN₃O₂

CAS No.

1216621-00-9

SMILES

O=C1N(CC)C2=CC=CC=C2N1C3=C(CO)CN(CC4CCCCCCC4)CC3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 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)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Trap-101Trap101Trap 101Opioid Receptornervous?systemparkinson's diseaseNOP receptorakinesiabradykinesiaInhibitorinhibitorinhibit

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:
Trap-101 hydrochloride
目录号:
HY-11052A
需求量: