WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H581952
CAS#: 2151842-64-5
Description: Zelquistinel, also known as AGN-241751 and GATE-251, is an orally active small-molecule NMDA receptor modulator which is under development for the treatment of major depressive disorder (MDD). Zelquistinel acts through a unique binding site on the NMDA receptor, independent of the glycine site, to modulate receptor activity and enhance NMDAR-mediated synaptic plasticity. Its mechanism of action is similar to that of rapastinel. However, unlike rapastinel, zelquistinel is orally bioavailable, exhibits increased potency, and has improved drug properties.
Hodoodo Cat#: H581952
Name: Zelquistinel
CAS#: 2151842-64-5
Chemical Formula: C15H25N3O5
Exact Mass: 327.18
Molecular Weight: 327.380
Elemental Analysis: C, 55.03; H, 7.70; N, 12.84; O, 24.43
Synonym: zelquistinel; AGN-241751; AGN 241751; AGN24175; GATE-251; GATE 251; GATE251;
IUPAC/Chemical Name: tert-butyl (4S)-2-[(2S,3R)-1-amino-3-hydroxy-1- oxobutan-2-yl]-1-oxo-2,5-diazaspiro[3.4]octane-5-carboxylate
InChi Key: ABAPCYNTEPGBNJ-FTGAXOIBSA-N
InChi Code: InChI=1S/C15H25N3O5/c1-9(19)10(11(16)20)17-8-15(12(17)21)6-5-7-18(15)13(22)23-14(2,3)4/h9-10,19H,5-8H2,1-4H3,(H2,16,20)/t9-,10+,15+/m1/s1
SMILES Code: O=C(N(CCC1)[C@@]21CN([C@@H]([C@H](O)C)C(N)=O)C2=O)OC(C)(C)C
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
Shelf Life: >3 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:
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The following data is based on the product molecular weight 327.38 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.
| 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 |
| Formulation protocol: | |
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| In vivo protocol: |
1: Fonteneau M, Brugoux A, Jaccaz D, Donello JE, Banerjee P, Le Merrer J, Becker JA. The NMDA receptor modulator zelquistinel durably relieves behavioral deficits in three mouse models of autism spectrum disorder. Neuropharmacology. 2024 May 1;248:109889. doi: 10.1016/j.neuropharm.2024.109889. Epub 2024 Feb 22. PMID: 38401792.
2: Burgdorf JS, Zhang XL, Stanton PK, Moskal JR, Donello JE. Zelquistinel Is an Orally Bioavailable Novel NMDA Receptor Allosteric Modulator That Exhibits Rapid and Sustained Antidepressant-Like Effects. Int J Neuropsychopharmacol. 2022 Dec 12;25(12):979-991. doi: 10.1093/ijnp/pyac043. PMID: 35882204; PMCID: PMC9743962.
