GNE-0723 | CAS#1883518-31-7 | NMDAR PAM

MedKoo Cat#: 522648 | Name: GNE-0723

Description:

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

GNE-0723 is a highly potent and brain penetrant GluN2A-selective NMDAR PAM suitable for in vivo characterization. EC50 (GluN2A) = 0.021 microM; EC50 (GluNA2 Flip) = 9.1 microM; EC50 (GluNA2 Flop) = 5.5 microM. The N-methyl-D-aspartate receptor (NMDAR) is a Na+ and Ca2+ permeable ionotropic glutamate receptor that is activated by the coagonists glycine and glutamate. NMDARs are critical to synaptic signaling and plasticity, and their dysfunction has been implicated in a number of neurologicaldisorders, including schizophrenia, depression, and Alzheimer’s disease.

Chemical Structure

GNE-0723

CAS#1883518-31-7

Theoretical Analysis

MedKoo Cat#: 522648

Name: GNE-0723

CAS#: 1883518-31-7

Chemical Formula: C16H8ClF6N5OS

Exact Mass: 467.0042

Molecular Weight: 467.77

Elemental Analysis: C, 41.08; H, 1.72; Cl, 7.58; F, 24.37; N, 14.97; O, 3.42; S, 6.85

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.

Bulk Inquiry

Related CAS #

No Data

Synonym

GNE-0723; GNE 0723; GNE0723.

IUPAC/Chemical Name

(1R,2R)-2-(7-((5-chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl)methyl)-5-oxo-2-(trifluoromethyl)-5H-thiazolo[3,2-a]pyrimidin-3-yl)cyclopropane-1-carbonitrile

InChi Key

FTIBNGABJNFFAI-POYBYMJQSA-N

InChi Code

InChI=1S/C16H8ClF6N5OS/c17-10-3-9(15(18,19)20)26-27(10)5-7-2-11(29)28-12(8-1-6(8)4-24)13(16(21,22)23)30-14(28)25-7/h2-3,6,8H,1,5H2/t6-,8+/m0/s1

SMILES Code

N#C[C@H]1[C@H](C2=C(C(F)(F)F)SC3=NC(CN4N=C(C(F)(F)F)C=C4Cl)=CC(N32)=O)C1

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

The N-methyl-D-aspartate receptor (NMDAR) is a Na+ and Ca2+ permeable ionotropic glutamate receptor that is activated by the coagonists glycine and glutamate. NMDARs are critical to synaptic signaling and plasticity, and their dysfunction has been implicated in a number of neurologicaldisorders, including schizophrenia, depression, and Alzheimer’s disease. CAS# for GNE-0732 is not listed as of 3/8/2016 Sci-Finder database listed below CAS# for GNE-0732 related isomers CAS# 1698904-15-2 is (1R,2S)-GNE-0732 isomer CAS# 1698904-16-3 is (1S,2R)-GNE-0732 isomer

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 467.77 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

1: Volgraf M, Sellers BD, Jiang Y, Wu G, Ly CQ, Villemure E, Pastor RM, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Sun L, Fu Y, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Reynen P, Herrington J, Gustafson A, Liu Y, Dirksen A, Dietz MG, Liu Y, Wang TM, Hanson J, Hackos D, Scearce-Levie K, Schwarz JB. Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design. J Med Chem. 2016 Feb 26. [Epub ahead of print] PubMed PMID: 26919761.