[CAS NO. 1048346-74-2] RO5166017

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Catalog:	HY-12699
Brand:	MCE
CAS:	1048346-74-2

Overview

MDL	MFCD22493512
Molecular Weight	219.28
Molecular Formula	C12H17N3O
SMILES	CCN(C1=CC=CC=C1)C[C@@H]2N=C(N)OC2

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

Summary

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 ^[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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 114.01 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.5604 mL	22.8019 mL	45.6038 mL
5 mM	0.9121 mL	4.5604 mL	9.1208 mL
10 mM	0.4560 mL	2.2802 mL	4.5604 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (11.40 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (11.40 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (11.40 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[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.

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