[CAS NO. 1048346-74-2] RO5166017
PRODUCTS SPECIFICATIONS [1048346-74-2]
DESCRIPTION [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 |
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
DMSO : 25 mg/mL ( 114.01 mM ; Need ultrasonic)
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 |
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.