2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Apimostinel

Apimostinel  (Synonyms: NRX-1074; AGN-241660)

Cat. No.: HY-102053 Purity: 98.78%
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Apimostinel (NRX-1074; AGN-241660) est un agoniste partiel de récepteur NMDA qui est oralement actif.

Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.

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

Apimostinel Chemical Structure

Apimostinel Chemical Structure

CAS No. : 1421866-48-9

Size Price Stock Quantity
5 mg USD 450 In-stock
10 mg USD 720 In-stock
25 mg USD 1450 In-stock
50 mg USD 2350 In-stock
100 mg USD 3760 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Apimostinel Related Antibodies

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AMPA Receptor NMDA Receptor Kainate Receptor

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist[1].

In Vitro

Apimostinel (NRX-1074) modulates the NMDA receptor in a similar fashion to GLYX-13, but has a synthetic modification to one of the amino acids, conferring increased potency and oral bioavailability[1].

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

Apimostinel Related Antibodies
In Vivo

In preclinical models the two compounds both appear to be highly efficacious across a number of CNS disorders[1].

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

503.59

Formula

C25H37N5O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H](O)[C@@H](C(N)=O)NC([C@@]1(CC2=CC=CC=C2)N(C([C@H]3N(C([C@H]([C@H](O)C)N)=O)CCC3)=O)CCC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 155 mg/mL (307.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 6.67 mg/mL (13.24 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9857 mL 9.9287 mL 19.8574 mL
5 mM 0.3971 mL 1.9857 mL 3.9715 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 7.75 mg/mL (15.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (77.5 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: ≥ 7.75 mg/mL (15.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (77.5 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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 (stored under nitrogen). 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
H2O / DMSO 1 mM 1.9857 mL 9.9287 mL 19.8574 mL 49.6436 mL
5 mM 0.3971 mL 1.9857 mL 3.9715 mL 9.9287 mL
10 mM 0.1986 mL 0.9929 mL 1.9857 mL 4.9644 mL
DMSO 15 mM 0.1324 mL 0.6619 mL 1.3238 mL 3.3096 mL
20 mM 0.0993 mL 0.4964 mL 0.9929 mL 2.4822 mL
25 mM 0.0794 mL 0.3971 mL 0.7943 mL 1.9857 mL
30 mM 0.0662 mL 0.3310 mL 0.6619 mL 1.6548 mL
40 mM 0.0496 mL 0.2482 mL 0.4964 mL 1.2411 mL
50 mM 0.0397 mL 0.1986 mL 0.3971 mL 0.9929 mL
60 mM 0.0331 mL 0.1655 mL 0.3310 mL 0.8274 mL
80 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6205 mL
100 mM 0.0199 mL 0.0993 mL 0.1986 mL 0.4964 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Apimostinel 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:

Apimostinel1421866-48-9NRX-1074 AGN-241660NRX1074NRX 1074AGN241660AGN 241660AGN-241660iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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