GLUT4 activator 1 is a novel and potent glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM.

Physicochemical Properties

Molecular Formula	C23H21FN4O3S
Molecular Weight	452.50
Exact Mass	452.131
CAS #	2253733-37-6
PubChem CID	138454789
Appearance	White to light yellow solid powder
LogP	3.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	9
Heavy Atom Count	32
Complexity	618
Defined Atom Stereocenter Count	0
SMILES	C1(CC(N)=O)=CC=C(NC2=NN=C(C3=CC=CC=C3OCCOC)C3SC=CC=32)C(F)=C1
InChi Key	GWLCNGUGZNFYHI-UHFFFAOYSA-N
InChi Code	InChI=1S/C23H21FN4O3S/c1-30-9-10-31-19-5-3-2-4-15(19)21-22-16(8-11-32-22)23(28-27-21)26-18-7-6-14(12-17(18)24)13-20(25)29/h2-8,11-12H,9-10,13H2,1H3,(H2,25,29)(H,26,28)
Chemical Name	2-[3-fluoro-4-[[7-[2-(2-methoxyethoxy)phenyl]thieno[2,3-d]pyridazin-4-yl]amino]phenyl]acetamide
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

References

[1]. Discovery of novel pyridazine derivatives as glucose transporter type 4 (GLUT4) translocation activators. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1785-1790.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~220.99 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.52 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 (5.52 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 saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (5.52 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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	2.2099 mL	11.0497 mL	22.0994 mL
	5 mM	0.4420 mL	2.2099 mL	4.4199 mL
	10 mM	0.2210 mL	1.1050 mL	2.2099 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.