1. GPCR/G Protein Neuronal Signaling
  2. Trace Amine-associated Receptor (TAAR) 5-HT Receptor Dopamine Receptor
  3. Ralmitaront

Ralmitaront  (Synonyms: RO6889450)

Cat. No.: HY-109157 Purity: 99.92%
Data Sheet Handling Instructions Technical Support

Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.

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

Ralmitaront Chemical Structure

Ralmitaront Chemical Structure

CAS No. : 2133417-13-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 366 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
1 mg USD 140 In-stock
5 mg USD 350 In-stock
10 mg USD 540 In-stock
25 mg USD 920 In-stock
50 mg USD 1288 In-stock
100 mg USD 1700 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ralmitaront

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder[1][2][3][4].

IC50 & Target[1]

TAAR1

 

In Vitro

Ralmitaront (0-30 µM, 70 min) displays lower efficacy and slower binding kinetics than Ulotaront at TAAR1, whereas at the 5-HT1AR and the D2 R, Ralmitaront lacks demonstrable activity[1].

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

Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT02699372Hoffmann-La Roche
Healthy Volunteer
March 21, 2016Phase 1
NCT04512066Hoffmann-La Roche
Schizophrenia, Schizoaffective Disorder
September 8, 2020Phase 2
NCT03669640Hoffmann-La Roche
Schizophrenia, Schizoaffective Disorder
December 4, 2018Phase 2
Molecular Weight

314.38

Formula

C17H22N4O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NNC(CC)=C1C)NC2=CC=C([C@H]3CNCCO3)C=C2

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 : 100 mg/mL (318.09 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 3.1809 mL 15.9043 mL 31.8086 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (7.95 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 (7.95 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 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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.92%

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 3.1809 mL 15.9043 mL 31.8086 mL 79.5216 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 mL 15.9043 mL
10 mM 0.3181 mL 1.5904 mL 3.1809 mL 7.9522 mL
15 mM 0.2121 mL 1.0603 mL 2.1206 mL 5.3014 mL
20 mM 0.1590 mL 0.7952 mL 1.5904 mL 3.9761 mL
25 mM 0.1272 mL 0.6362 mL 1.2723 mL 3.1809 mL
30 mM 0.1060 mL 0.5301 mL 1.0603 mL 2.6507 mL
40 mM 0.0795 mL 0.3976 mL 0.7952 mL 1.9880 mL
50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5904 mL
60 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3254 mL
80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9940 mL
100 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL
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Product Name:
Ralmitaront
Cat. No.:
HY-109157
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