RO5256390
Based on 3 publication(s) in Google Scholar
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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- Pureza: 98.75%
- No. CAS: 1043495-96-0
- Fòrmula: C13H18N2O
- Peso molecular:218.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RO5256390
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
18 nM
Compound: 18; RO5256390
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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
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[PMID: 26985297] |
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 (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.
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Animal Model:Wistar rats aged 45 days old with binge-like eating[2]
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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.
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Animal Model:C57BL/6J mice, NMRI mice, Sprague-Dawley rats, Long-Evans rats and Cynomolgus macaques[3]
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Dosage:0.03-3 mg/kg; 0.01-1 mg/kg; 1-30 mg/kg; 1-10 mg/kg; 0.3-3 mg/kg
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Administration:Oral administration (p.o.); 15min, 30 min or 60 min
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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.
Chemical Information
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No. CAS 1043495-96-0
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Appearance Solid
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Peso molecular 218.30
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Fòrmula C13H18N2O
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Color White to off-white
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SMILES
NC1=N[C@@H](C[C@@H](C2=CC=CC=C2)CC)CO1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Rep
The versatile binding landscape of the TAAR1 pocket for LSD and other antipsychotic drug molecules. [Abstract]2024 Jul 11;43(7):114505. PMID: 39002128 -
Mol Pharmacol
Trace amine-associated receptor 1 agonists differentially regulate dopamine transporter function. [Abstract]2025 Jul 28;107(9):100064. PMID: 40840012 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Barnes DA, et al. TAAR1 Regulates Purinergic-induced TNF Secretion from Peripheral, But Not CNS-resident, Macrophages. J Neuroimmune Pharmacol. 2023 Jun;18(1-2):100-111. [Content Brief]
[2]. Ferragud A, et al. The Trace Amine-Associated Receptor 1 Agonist RO5256390 Blocks Compulsive, Binge-like Eating in Rats. Neuropsychopharmacology. 2017 Jun;42(7):1458-1470. [Content Brief]
[3]. Revel FG, et al. A new perspective for schizophrenia: TAAR1 agonists reveal antipsychotic- and antidepressant-like activity, improve cognition and control body weight. Mol Psychiatry. 2013 May;18(5):543-56. [Content Brief]
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 |
RO5256390 Related Classifications
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