MedKoo Cat#: 526675 | Name: Apimostinel

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Apimostinel, also known as NRX-1074, also known as AGN-241660, is a novel antidepressant, acting as a selective partial agonist of an allosteric site of the glycine site of the NMDA receptor complex, which is under investigation by Naurex (recently acquired by Allergan) for the treatment of major depressive disorder. Its mechanism of action and effects are similar to those of rapastinel (GLYX-13), which is under development as an adjunctive therapy for treatment-resistant depression also by Naurex; however, NRX-1074 is 100-fold more potent by weight and, unlike GLYX-13 (which must be administered via intravenous injection), is orally-active.

Chemical Structure

Apimostinel
Apimostinel
CAS#1421866-48-9 (free base)

Theoretical Analysis

MedKoo Cat#: 526675

Name: Apimostinel

CAS#: 1421866-48-9 (free base)

Chemical Formula: C25H37N5O6

Exact Mass: 503.2744

Molecular Weight: 503.60

Elemental Analysis: C, 59.63; H, 7.41; N, 13.91; O, 19.06

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
Synonym
NRX-1074; NRX 1074; NRX1074; AGN-241660; AGN241660; AGN 241660. Apimostinel
IUPAC/Chemical Name
(2R)-1-[(2S)-1-[(2S,3R)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-2-benzylpyrrolidine-2-carboxamide
InChi Key
DVBUEXCIEIAXPM-PJUQSVSOSA-N
InChi Code
InChI=1S/C25H37N5O6/c1-15(31)19(26)23(35)29-12-6-10-18(29)22(34)30-13-7-11-25(30,14-17-8-4-3-5-9-17)24(36)28-20(16(2)32)21(27)33/h3-5,8-9,15-16,18-20,31-32H,6-7,10-14,26H2,1-2H3,(H2,27,33)(H,28,36)/t15-,16-,18+,19+,20+,25-/m1/s1
SMILES Code
O=C([C@@]1(CC2=CC=CC=C2)N(C([C@H]3N(C([C@@H](N)[C@H](O)C)=O)CCC3)=O)CCC1)N[C@@H]([C@H](O)C)C(N)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
NRX-1074 is intended by Naurex as an improved, follow-up drug to GLYX-13. The drug has shown rapid antidepressant effects in pre-clinical models of depression. In addition, similarly to GLYX-13, it is well-tolerated and lacks the schizophrenia-like psychotomimetic effects of other NMDA receptor antagonists such as ketamine. As of 2015, an intravenous formulation of NRX-1074 is in a phase II clinical trial for MDD, and an oral formulation is concurrently in phase I trials for MDD.

Preparing Stock Solutions

The following data is based on the product molecular weight 503.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Park M, Niciu MJ, Zarate CA Jr. Novel Glutamatergic Treatments for Severe Mood Disorders. Curr Behav Neurosci Rep. 2015 Dec;2(4):198-208. Epub 2015 Oct 9. PubMed PMID: 26824031; PubMed Central PMCID: PMC4725605. 2: Javelot H. [Psychopharmacology of anxiety and depression: Historical aspects, current treatments and perspectives]. Ann Pharm Fr. 2016 Mar;74(2):93-118. doi: 10.1016/j.pharma.2015.09.001. Epub 2015 Oct 16. Review. French. PubMed PMID: 26472602.