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RO5166017

Catalog No. T34373 CAS 1048346-74-2

Synonyms: RO 5166017, RO-5166017

RO5166017 is an orally active, potent and selective trace amine-associated receptor 1 (TAAR1) agonist for the study of conditioned taste aversion frontal nerve disorders.

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RO5166017, CAS 1048346-74-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 98.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 652.00
50 mg	In stock	$ 913.00
100 mg	In stock	$ 1,230.00
500 mg	In stock	$ 2,460.00

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Purity: 99.84%

Biological Description

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Description	RO5166017 is an orally active, potent and selective trace amine-associated receptor 1 (TAAR1) agonist for the study of conditioned taste aversion frontal nerve disorders.
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[2].
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[2].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[2].RO5166017 prevents cocaine-induced hyperlocomotion and inhibits cocaine-induced stereotypies in WT mice, similar to olanzapine, an effect that disappears in Taar1 mice[1].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[1]. Chronic treatment of diet-induced obese (DIO) mice with RO5166017 reduces food intake and body weight[1].

Synonyms	RO 5166017, RO-5166017
Molecular Weight	219.28
Formula	C12H17N3O
CAS No.	1048346-74-2

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/mL (91.21 mM), Sonication is recommended.

References and Literature

1. 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. 2. Revel FG,et al. TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A. 2011 May 17;108(20):8485-90. 3. Cichero E, Espinoza S, Franchini S, Guariento S, Brasili L, Gainetdinov RR, Fossa P. Further insights into the pharmacology of the human trace amine-associated receptors: discovery of novel ligands for TAAR1 by a virtual screening approach. Chem Biol Drug Des. 2014 Dec;84(6):712-20. doi: 10.1111/cbdd.12367. Epub 2014 Jun 30. PubMed PMID: 24894156. 4. Leo D, Mus L, Espinoza S, Hoener MC, Sotnikova TD, Gainetdinov RR. Taar1-mediated modulation of presynaptic dopaminergic neurotransmission: role of D2 dopamine autoreceptors. Neuropharmacology. 2014 Jun;81:283-91. doi: 10.1016/j.neuropharm.2014.02.007. Epub 2014 Feb 22. PubMed PMID: 24565640.

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Keywords

RO5166017 1048346-74-2 Others RO 5166017 RO5166017 HCl RO-5166017 inhibitor inhibit

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