[CAS NO. 1421866-48-9] Apimostinel

Name: Apimostinel
Brand: Arctom Scientific
SKU: AS946462

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PRODUCTS SPECIFICATIONS [1421866-48-9]

Distributor

Catalog

AS946462

Brand

Arctom Scientific

CAS

1421866-48-9

DESCRIPTION [1421866-48-9]

Overview

MDL	-
Molecular Weight	503.59
Molecular Formula	C25H37N5O6
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

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

Summary

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] .

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

In Vivo

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

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01856556	Naurex, Inc, an affiliate of Allergan plc	Healthy	May 2013	Phase 1
NCT05597241	Gate Neurosciences, Inc	Major Depressive Disorder	October 15, 2022	Phase 1
NCT02067793	Naurex, Inc, an affiliate of Allergan plc	Major Depressive Disorder	March 2014	Phase 2
NCT02603458	NYU Langone Health\|Naurex, Inc, an affiliate of Allergan plc	Schizophrenia		Phase 2
NCT02366364	Naurex, Inc, an affiliate of Allergan plc	Major Depressive Disorder	February 2015	Phase 1

Appearance

Solid

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)

H ₂ O : ≥ 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
10 mM	0.1986 mL	0.9929 mL	1.9857 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
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

* All of the co-solvents are available by MCE.

References

[1] Naurex's First Orally Active Molecule, NRX-1074, Demonstrates Statistically Significant Improvement in Depression Scores within 24 Hours in Phase 2 Study for Major Depressive Disorder. January 28, 2015.