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Über diesen Artikel
Empirische Formel (Hill-System):
C12H17N3O
CAS-Nummer:
Molekulargewicht:
219.28
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
powder
Preise und Verfügbarkeit sind derzeit nicht verfügbar.
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Unterstützung erhaltenQuality Segment
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
SMILES string
N1[C@H](COC1=N)CN(CC)c2ccccc2
InChI key
PPONHQQJLWPUPH-JTQLQIEISA-N
Biochem/physiol Actions
Orally active, high-affinity, potent and selective trace amine-associated receptor 1 (TAAR1) agonist with antipsychotic-like efficacy in vivo.
RO5166017 is an orally active, high-affinity, potent and selective trace amine-associated receptor 1 (TAAR1) agonist (mouse/rat/human/monkey Ki = 1.9/2.7/31/24 nM, cAMP EC50 = 3.3/14/55/97 nM using respective HEK293 transfectants; GIRK EC50 = 8 nM with mTAAR1-expressing Xenopus oocytes; neurons firing frequency IC50 = 1.73/2.99 nM in mouse VTA/DRN slices) with good selectivity over TAAR4 and 123 other proteins. RO5166017 reduces spontaneous hyperlocomotion in Dat-/- mice (0.5 mg/kg ip.), as well as hyperlocomotion induction by cocaine or NMDAR agonist L-687,414 in wild-type (0.01-0.3 mg/kg po.), but not Taar1-knockout mice.
RO5166017 is an orally active, high-affinity, potent and selective trace amine-associated receptor 1 (TAAR1) agonist (mouse/rat/human/monkey Ki = 1.9/2.7/31/24 nM, cAMP EC50 = 3.3/14/55/97 nM using respective HEK293 transfectants; GIRK EC50 = 8 nM with mTAAR1-expressing Xenopus oocytes; neurons firing frequency IC50 = 1.73/2.99 nM in mouse VTA/DRN slices) with good selectivity over TAAR4 and 123 other proteins. RO5166017 reduces spontaneous hyperlocomotion in Dat-/- mice (0.5 mg/kg ip.), as well as hyperlocomotion induction by cocaine or NMDAR agonist L-687,414 in wild-type (0.01-0.3 mg/kg po.), but not Taar1-knockout mice.
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Dieser Artikel | ||
|---|---|---|
| description ≥95% (HPLC) | description ≥98% (HPLC) | description ≥98% (HPLC) |
| form powder | form solid | form powder |
| assay ≥95% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| Quality Level 100 | Quality Level 100 | Quality Level 100 |
| storage temp. -10 to -25°C | storage temp. 2-8°C | storage temp. 2-8°C |
| solubility DMSO: 2 mg/mL, clear | solubility DMSO: 2 mg/mL, clear | solubility H2O: 2 mg/mL, clear |
| color white to beige | color white to beige | color white to beige |
Lagerklasse
11 - Combustible Solids
Flammpunkt (°F)
Not applicable
Flammpunkt (°C)
Not applicable
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