SML3477

RO5166017

≥95% (HPLC)

• Synonym(e): (4S)-2-Amino-N-ethyl-4,5-dihydro-N-phenyl-4-oxazolemethanamine, (S)-4-((Ethyl(phenyl)amino)methyl)-4,5-dihydrooxazol-2-amine
• Empirische Formel (Hill-System): C₁₂H₁₇N₃O
• CAS-Nummer: 1048346-74-2
• Molekulargewicht: 219.28
• MDL-Nummer: MFCD22493512
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: -10 to -25°C

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable