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製品番号: HY-11052A

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Trap-101 hydrochloride

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ³⁵S binding to CHO_hNOP membranes with pK_i 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 1216621-00-9
分子式: C₂₄H₃₆ClN₃O₂
分子量:434.01

保管条件:

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

Data Sheet (277 KB)

Trap-101 hydrochloride 構造式

CAS 番号: 1216621-00-9

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
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関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

NOP Receptor/ORL1

Opioid Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

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 (pK_i 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].

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

体内実験

Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in na ve 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].

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

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.

化学情報

CAS 番号 1216621-00-9
分子量 434.01
分子式 C₂₄H₃₆ClN₃O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Matteo Marti, et al. The novel nociceptin/orphanin FQ receptor antagonist Trap-101 alleviates experimental parkinsonism through inhibition of the nigro-thalamic pathway: positive interaction with L-DOPA. J Neurochem. 2008 Dec;107(6):1683-96. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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生物活性
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- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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Trap-101 hydrochloride

Opioid Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Trap-101 hydrochloride 関連分類

HY-11052A 関連分類