RO5166017 是具有口服活性的、跨物种的 TAAR1 的激动剂，其对小鼠、大鼠、人和食蟹猴的 K_i 值分别为1.9 nM、2.7 nM、31 nM 和 24 nM。

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

Solid

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

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.
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..
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.
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. Subchronic treatment of diet-induced obese (DIO) mice with RO5166017 results in reduced food intake and body weight.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Florent G Revel, et al. TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A
[2]. Justin N Siemian, et al. Trace amine-associated receptor 1 agonists RO5263397 and RO5166017 attenuate quinpirole-induced yawning but not hypothermia in rats. Behav Pharmacol. 2017 Oct;28(7):590-593.

In Vitro: DMSO : 25 mg/mL (114.01 mM; Need ultrasonic)配制储备液