2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)
  4. RO5263397

RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.

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RO5263397 Chemical Structure

RO5263397 Chemical Structure

CAS No. : 1357266-05-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

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RO5263397 Related Antibodies

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  • Purity & Documentation

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Description

RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
17 nM
Compound: 48; RO5263397
Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
[PMID: 26985297]
HEK293 EC50
35 nM
Compound: 48; RO5263397
Agonist activity at rat TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
Agonist activity at rat TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
[PMID: 26985297]
In Vivo

RO5263397 (0.1-1.0 mg/kg; p.o.; dosing at the mid-light phase (ZT6)) increases wake time at 0.3 and 1 mg/kg[2].
RO5263397 (0.3 and 1.0 mg/kg; p.o.) decreases NREM time in WT mice. RO5263397 (0.3 and 1.0 mg/kg; p.o.; in OE mice) powerfully increases W time in OE mice for 5-6 h. NREM sleep is suppressed for 4-6 h and REM sleep is almost completely suppressed for 6 h after all doses of RO5263397[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult 4-5-month-old male WT littermates (C57BL/6 background)[2]
Dosage: 0.1, 0.3, 1 mg/kg
Administration: p.o.; dosing at the mid-light phase (ZT6) 
Result: Increased wake time at 0.3 and 1 mg/kg
Molecular Weight

194.21

Formula

C10H11FN2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C([C@@H]2N=C(N)OC2)C=CC=C1F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 260 mg/mL (1338.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.1491 mL 25.7453 mL 51.4907 mL
5 mM 1.0298 mL 5.1491 mL 10.2981 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 6.5 mg/mL (33.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (65.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 6.5 mg/mL (33.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (65.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.1491 mL 25.7453 mL 51.4907 mL 128.7266 mL
5 mM 1.0298 mL 5.1491 mL 10.2981 mL 25.7453 mL
10 mM 0.5149 mL 2.5745 mL 5.1491 mL 12.8727 mL
15 mM 0.3433 mL 1.7164 mL 3.4327 mL 8.5818 mL
20 mM 0.2575 mL 1.2873 mL 2.5745 mL 6.4363 mL
25 mM 0.2060 mL 1.0298 mL 2.0596 mL 5.1491 mL
30 mM 0.1716 mL 0.8582 mL 1.7164 mL 4.2909 mL
40 mM 0.1287 mL 0.6436 mL 1.2873 mL 3.2182 mL
50 mM 0.1030 mL 0.5149 mL 1.0298 mL 2.5745 mL
60 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1454 mL
80 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6091 mL
100 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2873 mL
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RO5263397 Related Classifications

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.

Keywords:

RO52633971357266-05-7RO 5263397RO-5263397Trace Amine-associated Receptor (TAAR)wakefulnessspectralNREMREMsleeprhythmsantidepressantpsychiatricInhibitorinhibitorinhibit

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