2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)
  4. RO5256390

RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages.

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RO5256390 Chemical Structure

RO5256390 Chemical Structure

CAS No. : 1043495-96-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 170 In-stock
25 mg USD 340 In-stock
50 mg USD 540 In-stock
100 mg USD 770 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
18 nM
Compound: 18; RO5256390
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]
In Vitro

RO5256390 (0-100 nM; 0-6 h) inhibits ATP (HY-B2176) -induced TNF secretion in mouse bone marrow-derived macrophages in a concentration-dependent manner (IC50 : 19.8 nM), but has no effect on IL-6 secretion[1].
RO5256390 (0-100 nM; 0-6 h) has no effect on TNF and IL-6 secretion in ADP (HY-W010918) -induced mouse microglia[1].

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

RO5256390 Related Antibodies
In Vivo

RO5256390 (0-15 μg Intracranial administration for 10 minutes; 0-10 mg/kg Intraperitoneal injection for 30 minutes; Single dose) can block compulsive overeating behavior in rats[2].
RO5256390 (0.03-30 mg/kg; Oral administration; 15-60 minutes) exhibits pro-cognitive and antidepressant-like properties in rodent and primate models. RO5256390 produces a brain activation pattern reminiscent of Olanzapine (HY-14541) in rodents[3].

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

Animal Model: Wistar rats aged 45 days old with binge-like eating[2]
Dosage: 0, 1.5, 5 and 15 μg per side;
0, 1, 3, 10 mg/kg
Administration: Intracranial administration (ICV); 10 min prior to the operant sessions;
Intraperitoneal injection (i.p.); 30 min prior to the operant sessions
Result: Blocked binge-like eating in rats responding 1 h per day for a highly palatable sugary diet.
Selectively reduced the rate and regularity of palatable food responding, but it did not affect either baseline intake or food restriction-induced overeating of the standard chow diet.
Fully blocked compulsive-like eating when the palatable diet was offered in an aversive compartment of a light/dark conflict box, and blocked the conditioned rewarding properties of palatable food, as well as palatable food-seeking behavior in a second-order schedule of reinforcement.
Animal Model: C57BL/6J mice, NMRI mice, Sprague-Dawley rats, Long-Evans rats and Cynomolgus macaques[3]
Dosage: 0.03-3 mg/kg; 0.01-1 mg/kg; 1-30 mg/kg; 1-10 mg/kg; 0.3-3 mg/kg
Administration: Oral administration (p.o.); 15min, 30 min or 60 min
Result: Blocked psychostimulant-induced hyperactivity.
Did not induce cataplexy or weight gain.
Improved cognitive performance in cynomolgus macaques.
Inhibited psychostimulant induced hyperactivity.
Reversed cognitive deficits in rats.
Molecular Weight

218.30

Formula

C13H18N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=N[C@@H](C[C@@H](C2=CC=CC=C2)CC)CO1
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 : 50 mg/mL (229.04 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 4.5809 mL 22.9043 mL 45.8085 mL
5 mM 0.9162 mL 4.5809 mL 9.1617 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)

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (11.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (11.45 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

Purity: 98.75%

SDS (251 KB)

COA (249 KB) HNMR (254 KB) RP-HPLC (271 KB) MS (178 KB)

Handling Instructions (2659 KB)
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 4.5809 mL 22.9043 mL 45.8085 mL 114.5213 mL
5 mM 0.9162 mL 4.5809 mL 9.1617 mL 22.9043 mL
10 mM 0.4581 mL 2.2904 mL 4.5809 mL 11.4521 mL
15 mM 0.3054 mL 1.5270 mL 3.0539 mL 7.6348 mL
20 mM 0.2290 mL 1.1452 mL 2.2904 mL 5.7261 mL
25 mM 0.1832 mL 0.9162 mL 1.8323 mL 4.5809 mL
30 mM 0.1527 mL 0.7635 mL 1.5270 mL 3.8174 mL
40 mM 0.1145 mL 0.5726 mL 1.1452 mL 2.8630 mL
50 mM 0.0916 mL 0.4581 mL 0.9162 mL 2.2904 mL
60 mM 0.0763 mL 0.3817 mL 0.7635 mL 1.9087 mL
80 mM 0.0573 mL 0.2863 mL 0.5726 mL 1.4315 mL
100 mM 0.0458 mL 0.2290 mL 0.4581 mL 1.1452 mL
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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.

Keywords:

RO52563901043495-96-0RO 5256390RO-5256390Trace Amine-associated Receptor (TAAR)Anti-depressionTAAR1MacrophagesOvereating behavior modelInhibitorinhibitorinhibit

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