1048346-74-2
1048346-74-2 structure
- Name: RO 5166017
- Chemical Name: RO5166017
- CAS Number: 1048346-74-2
- Molecular Formula: C12H17N3O
- Molecular Weight: 219.28
- Catalog: Research Areas Metabolic Disease
- Create Date: 2018-06-21 16:17:24
- Modify Date: 2024-01-05 21:28:54
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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].
| Name | RO5166017 |
|---|---|
| Synonyms |
MFCD22493512
4-Oxazolidinemethanamine, N-ethyl-2-imino-N-phenyl-, (4S)- N-Ethyl-N-{[(4S)-2-imino-1,3-oxazolidin-4-yl]methyl}aniline RO5166017 |
| 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]. |
|---|---|
| Related Catalog | |
| 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]. |
| 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]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 314.7±34.0 °C at 760 mmHg |
| Molecular Formula | C12H17N3O |
| Molecular Weight | 219.28 |
| Flash Point | 144.2±25.7 °C |
| Exact Mass | 219.137161 |
| LogP | 1.32 |
| Vapour Pressure | 0.0±0.7 mmHg at 25°C |
| Index of Refraction | 1.589 |
| Storage condition | -20°C |