RO5166017

SKU: orb1695431

Description

RO5166017 is a potent, selective, and orally bioavailable TAAR1 agonist used in neuroscience research. It serves as a valuable tool compound for investigating trace amine-associated receptor 1 function in preclinical models, including studies on neuropsychiatric and neurological disorders in both in vitro and in vivo systems.

Key Properties

• CAS Number: 1048346-74-2
• MW: 219.28
• Purity: 99.84%
• Formula: C₁₂H₁₇N₃O
• SMILES: CCN(C[C@H]1COC(N)=N1)c1ccccc1
• Target: Others
• Solubility: DMSO:20 mg/mL (91.21 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (9.12 mM)

Bioactivity

• In Vivo:
  RO5166017 prevents stress-induced hyperthermia and blocks dopamine-dependent hyperlocomotion in cocaine-treated and dopamine transporter knockout mice, as well as NMDA antagonist-induced hyperactivity.Administered orally at doses of 0.01-1 mg/kg, RO5166017 dose-dependently prevents stress-induced hyperthermia in NMRI mice. At doses of 0.1-0.3 mg/kg, RO5166017 exhibits TAAR1-mediated anxiolytic-like properties.RO5166017 prevents cocaine-induced hyperlocomotion and inhibits cocaine-induced stereotypies in WT mice, similar to olanzapine, an effect that disappears in Taar1 mice.Activation of TAAR1 by RO5166017 increases glucose-dependent insulin secretion in INS1E cells and human islets, and elevates plasma levels of peptide YY (PYY) and glucagon-like peptide 1 (GLP-1) in mice. Chronic treatment of diet-induced obese (DIO) mice with RO5166017 reduces food intake and body weight.
• In Vitro:
  RO5166017 exhibits high affinity and potent functional activity against mouse/rat/cynomolgus/human TAAR1 stably expressed in HEK293 cells and demonstrates high selectivity relative to other targets.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAAR1, RO 5166017, RO5166017, RO-5166017, RO5166017 HCl

Compound Identifiers

PubChem CID

25016538