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MedKoo Cat#: 555180 | Name: GNE-8324
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Description:

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

GNE-8324 is a potent and selective NMDA receptor PAM.

Chemical Structure

GNE-8324
GNE-8324
CAS#1698901-76-6

Theoretical Analysis

MedKoo Cat#: 555180

Name: GNE-8324

CAS#: 1698901-76-6

Chemical Formula: C18H18FN3OS

Exact Mass: 343.1155

Molecular Weight: 343.42

Elemental Analysis: C, 62.95; H, 5.28; F, 5.53; N, 12.24; O, 4.66; S, 9.34

Price and Availability

Size Price Availability Quantity
5mg USD 950.00 2 Weeks
10mg USD 1,550.00 2 Weeks
500mg USD 3,650.00 2 Weeks
1g USD 5,650.00 2 Weeks
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Related CAS #
No Data
Synonym
GNE-8324; GNE 8324; GNE8324
IUPAC/Chemical Name
2-((ethyl(4-fluorophenyl)amino)methyl)-7,8-dihydro-4H,6H-cyclopenta[4,5]thiazolo[3,2-a]pyrimidin-4-one
InChi Key
MKBFOAQLSFHEGN-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H18FN3OS/c1-2-21(14-8-6-12(19)7-9-14)11-13-10-17(23)22-15-4-3-5-16(15)24-18(22)20-13/h6-10H,2-5,11H2,1H3
SMILES Code
O=C1C=C(CN(CC)C2=CC=C(F)C=C2)N=C3N1C(CCC4)=C4S3
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
>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
NMDA Receptors (NMDARs) play key roles in synaptic physiology and NMDAR hypofunction has been implicated in various neurological conditions.
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons.
In vitro activity:
This study showed previously that NMDAR positive allosteric modulator GNE-8324 and M-8324 selectively increase NMDAR activity on the inhibitory neurons and elevates their activity in vitro and in vivo. Reference: Front Pharmacol. 2022 Jan 4;12:796179. https://pubmed.ncbi.nlm.nih.gov/35058780/
In vivo activity:
Interestingly, a significant increase in the frequency of sIPSC was also seen in mice infused with M-8324 (derivative of GNE-8324) (Fig. 5G), consistent with an increased presynaptic activity-driven enhancement in inhibition by M-8324 which may prevent the occurrence of tinnitus. Reference: Nat Commun. 2018 Oct 1;9(1):4000. https://pubmed.ncbi.nlm.nih.gov/30275542/

Preparing Stock Solutions

The following data is based on the product molecular weight 343.42 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
Formulation protocol:
2. Deng D, Masri S, Yao L, Ma X, Cao X, Yang S, Bao S, Zhou Q. Increasing endogenous activity of NMDARs on GABAergic neurons increases inhibition, alters sensory processing and prevents noise-induced tinnitus. Sci Rep. 2020 Jul 20;10(1):11969. doi: 10.1038/s41598-020-68652-5. PMID: 32686710; PMCID: PMC7371882. 3. Yao L, Grand T, Hanson JE, Paoletti P, Zhou Q. Higher ambient synaptic glutamate at inhibitory versus excitatory neurons differentially impacts NMDA receptor activity. Nat Commun. 2018 Oct 1;9(1):4000. doi: 10.1038/s41467-018-06512-7. Erratum in: Nat Commun. 2018 Nov 15;9(1):4887. PMID: 30275542; PMCID: PMC6167324.
In vitro protocol:
1. Xia D, Zhang X, Deng D, Ma X, Masri S, Wang J, Bao S, Hu S, Zhou Q. Long-Term Enhancement of NMDA Receptor Function in Inhibitory Neurons Preferentially Modulates Potassium Channels and Cell Adhesion Molecules. Front Pharmacol. 2022 Jan 4;12:796179. doi: 10.3389/fphar.2021.796179. PMID: 35058780; PMCID: PMC8764260.
In vivo protocol:
1. Deng D, Masri S, Yao L, Ma X, Cao X, Yang S, Bao S, Zhou Q. Increasing endogenous activity of NMDARs on GABAergic neurons increases inhibition, alters sensory processing and prevents noise-induced tinnitus. Sci Rep. 2020 Jul 20;10(1):11969. doi: 10.1038/s41598-020-68652-5. PMID: 32686710; PMCID: PMC7371882. 2. Yao L, Grand T, Hanson JE, Paoletti P, Zhou Q. Higher ambient synaptic glutamate at inhibitory versus excitatory neurons differentially impacts NMDA receptor activity. Nat Commun. 2018 Oct 1;9(1):4000. doi: 10.1038/s41467-018-06512-7. Erratum in: Nat Commun. 2018 Nov 15;9(1):4887. PMID: 30275542; PMCID: PMC6167324.
1: Hackos DH, Hanson JE. Diverse modes of NMDA receptor positive allosteric modulation: Mechanisms and consequences. Neuropharmacology. 2017 Jan;112(Pt A):34-45. doi: 10.1016/j.neuropharm.2016.07.037. Epub 2016 Jul 30. Review. PubMed PMID: 27484578.