PeptideDB

GET73 202402-01-5

GET73 202402-01-5

CAS No.: 202402-01-5

GET73 is an analog of the natural neurotransmitter gamma-hydroxybutyrate (GHB). GET73 has anti-alcohol and anxiolytic (a
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

GET73 is an analog of the natural neurotransmitter gamma-hydroxybutyrate (GHB). GET73 has anti-alcohol and anxiolytic (anti-anxiety) properties. GET73 has significant effects on glutamate transmission in the hippocampus.

Physicochemical Properties


Molecular Formula C₁₃H₁₆F₃NO₂
Molecular Weight 275.27
Exact Mass 275.113
CAS # 202402-01-5
PubChem CID 10221200
Appearance White to off-white solid powder
LogP 3.588
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 6
Heavy Atom Count 19
Complexity 274
Defined Atom Stereocenter Count 0
SMILES

FC(C1C=CC(=CC=1)CNC(CCCOC)=O)(F)F

InChi Key QLZOWJNFLXSDSH-UHFFFAOYSA-N
InChi Code

InChI=1S/C13H16F3NO2/c1-19-8-2-3-12(18)17-9-10-4-6-11(7-5-10)13(14,15)16/h4-7H,2-3,8-9H2,1H3,(H,17,18)
Chemical Name

4-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]butanamide
Synonyms

GET-73; GET 73
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro One hour before and after chronic ethanol exposure, GET73 (1 µM, 10 µM; 1 hour) guards against ethanol-induced reductions in cell viability, cytoskeletal changes, lower extracellular glutamate levels, and enhanced reactive oxygen species formation [1].
ln Vivo The elevated plus maze (EPM) test in Sprague-Dawley rats exposed to GET73 (5–50 mg/kg; ir) results in anxiolytic effects [3].
Cell Assay Cell Viability Assay[1]
Cell Types: Rat Hippocampal Neurons
Tested Concentrations: 0.1 µM, 1 µM, 10 µM
Incubation Duration: 1 hour
Experimental Results: Prevention of ethanol (75 mM, 4 days)-induced decrease in MTT.
Animal Protocol Animal/Disease Models: Male SD rat (200-300 g and 300-350 g) [3]
Doses: 5 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg
Route of Administration: po (oral gavage)
Experimental Results: Exerts anxiolytic effects in rats exposed to the elevated plus maze (EPM) test.
References [1]. Tomasini MC, et al. GET73 Prevents Ethanol-Induced Neurotoxicity in Primary Cultures of Rat Hippocampal Neurons. Alcohol Alcohol. 2016 Mar;51(2):128-35.
[2]. Ferraro L, et al. GET73 modulates rat hippocampal glutamate transmission: evidence for a functional interaction with mGluR5. Pharmacol Rep. 2011;63(6):1359-71.
[3]. Loche A, et al. Anti-Alcohol and Anxiolytic Properties of a New Chemical Entity, GET73. Front Psychiatry. 2012 Feb 14;3:8.
Additional Infomation Get 73 has been investigated for the treatment of Alcohol Dependence.

Solubility Data


Solubility (In Vitro) DMSO : ~100 mg/mL (~363.28 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 3: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6328 mL 18.1640 mL 36.3280 mL
5 mM 0.7266 mL 3.6328 mL 7.2656 mL
10 mM 0.3633 mL 1.8164 mL 3.6328 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.