1. GPCR/G Protein
  2. Trace Amine-associated Receptor (TAAR)
  3. RO5166017

RO5166017 

Cat. No.: HY-12699 Purity: 99.48%
COA Handling Instructions

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.

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

RO5166017 Chemical Structure

RO5166017 Chemical Structure

CAS No. : 1048346-74-2

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5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 960 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1540 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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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].

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.

Molecular Weight

219.28

Formula

C12H17N3O

CAS No.
SMILES

CCN(C1=CC=CC=C1)C[[email protected]@H]2N=C(N)OC2

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.
Purity & Documentation

Purity: 99.48%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
RO5166017
Cat. No.:
HY-12699
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