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ChemicalBook--->CAS DataBase List--->1216621-00-9

1216621-00-9

1216621-00-9 Structure

1216621-00-9 Structure
IdentificationBack Directory
[Name]

1-(1-(cyclooctylMethyl)-5-(hydroxyMethyl)-1,2,3,6-tetrahydropyridin-4-yl)-3-ethyl-1H-benzo[d]iMidazol-2(3H)-one hydrochloride
[CAS]

1216621-00-9
[Synonyms]

Trap-101 hydrochloride
Trap-101 hydrochloride >=98% (HPLC), powder
1-[1-(cyclooctylmethyl)-5-(hydroxymethyl)-3,6-dihydro-2H-pyridin-4-yl]-3-ethylbenzimidazol-2-one:hydrochloride
1-(1-(cyclooctylMethyl)-5-(hydroxyMethyl)-1,2,3,6-tetrahydropyridin-4-yl)-3-ethyl-1H-benzo[d]iMidazol-2(3H)-one hydrochloride
[Molecular Formula]

C24H36ClN3O2
[MDL Number]

MFCD09971083
[MOL File]

1216621-00-9.mol
[Molecular Weight]

434.015
Chemical PropertiesBack Directory
[storage temp. ]

2-8°C
[solubility ]

H2O: ≥10mg/mL
[form ]

powder
[color ]

white to off-white
Safety DataBack Directory
[Hazard Codes ]

T
[Risk Statements ]

25
[Safety Statements ]

45
[RIDADR ]

UN 2811 6.1 / PGIII
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

Trap 101 is a useful intermediate and used to study protein-coupled receptor
[Biological Activity]

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors, with selectivity for NOP receptors over other opioid receptors. Trap-101 stimulated GTPγ35S binding to CHOhNOP 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 Parkinson's disease rats and can be used for neurological disease research.
[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 (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.

[target]

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

[storage]

Store at -20°C
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