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RO5166017 

Cat. No.: HY-12699
Handling Instructions

RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.

For research use only. We do not sell to patients.

RO5166017 Chemical Structure

RO5166017 Chemical Structure

CAS No. : 1048346-74-2

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Description

RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively[1].

In Vitro

RO5166017 showed high affinity and potent functional activity at mouse, rat, cynomolgus monkey, and human TAAR1 stably expressed in HEK293 cells as well as high selectivity vs. other targets[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RO5166017 prevents stress-induced hyperthermia and blocked dopamine-dependent hyperlocomotion in cocaine-treated and dopamine transporter knockout mice as well as hyperactivity induced by an NMDA antagonist[1].
RO5166017 (0.01-1 mg/kg, orally) dose-dependently prevents the SIH in NMRI mice. RO5166017 exhibits TAAR1-mediated anxiolytic-like properties at doses 0.1-0.3 mg/kg.[1].
RO5166017 prevents the cocaine-induced hyperlocomotion. RO5166017 also inhibits stereotypies induced by cocaine in WT mice similar to olanzapine, and this effect is lost in Taar1−/− mice[1].
TAAR1 activation by RO5166017 increases glucose-dependent insulin secretion in INS1E cells and human islets and elevated plasma and peptide YY (PYY) and glucagon like peptide 1 (GLP-1) levels in mice[2]. Subchronic treatment of diet-induced obese (DIO) mice with RO5166017 results in reduced food intake and body weight[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

219.28

Formula

C₁₂H₁₇N₃O

CAS No.
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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RO5166017
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HY-12699
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