Identification | Back 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 |
Hazard Information | Back 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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