EAAT2 activator 1 is a potent activator of excitatory amino acid (AA) transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels in a dose-dependent manner.

Physicochemical Properties

Molecular Formula	C16H11CLFN3S
Molecular Weight	331.795044183731
Exact Mass	331.034
CAS #	892415-28-0
PubChem CID	20900510
Appearance	Light brown to brown solid powder
LogP	3.5
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	4
Heavy Atom Count	22
Complexity	349
Defined Atom Stereocenter Count	0
SMILES	FC1C(CSC2C=CC(C3C=CC=CN=3)=NN=2)=C(Cl)C=CC=1
InChi Key	DCLFFJASADCESO-UHFFFAOYSA-N
InChi Code	InChI=1S/C16H11ClFN3S/c17-12-4-3-5-13(18)11(12)10-22-16-8-7-15(20-21-16)14-6-1-2-9-19-14/h1-9H,10H2
Chemical Name	3-[(2-chloro-6-fluorophenyl)methylsulfanyl]-6-pyridin-2-ylpyridazine
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

Targets	EAAT2
References	[1]. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators. Bioorg Med Chem Lett. 2011;21(19):5774-5777.

Solubility Data

Solubility (In Vitro)

DMSO: 25 mg/mL (75.35 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 1.67 mg/mL (5.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.0139 mL	15.0693 mL	30.1386 mL
	5 mM	0.6028 mL	3.0139 mL	6.0277 mL
	10 mM	0.3014 mL	1.5069 mL	3.0139 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.