HIF-2α Agonist 2 (Compound 10) is a HIF-2α agonist/activator with EC50 of 1.68 μM at a dose of 20 μM. HIF-2α agonist 2 has no cytotoxic effect on 786-O-HRE-Luc cells. 2α agonist 2 may be utilized in oxygen consumption studies.

Physicochemical Properties

Molecular Formula	C13H8BR2N2O2S
Molecular Weight	416.087820053101
Exact Mass	415.865
CAS #	2750141-15-0
PubChem CID	164617432
Appearance	White to off-white solid powder
LogP	3.1
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	2
Heavy Atom Count	20
Complexity	493
Defined Atom Stereocenter Count	0
InChi Key	NYIUNIQAWCQVNX-UHFFFAOYSA-N
InChi Code	InChI=1S/C13H8Br2N2O2S/c14-8-5-9(15)7-10(6-8)16-13-11-3-1-2-4-12(11)20(18,19)17-13/h1-7H,(H,16,17)
Chemical Name	N-(3,5-dibromophenyl)-1,1-dioxo-1,2-benzothiazol-3-amine
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	HIF-2 must be activated by HIF-2α agonist 2 (0.001-100 μM; 24 h), which has an EC50 value of 1.68 μM at a dose of 20 μM [1]. Agonist for HIF-2α 2 (0.003–20 μM; 24 hours).
Cell Assay	Cell viability assay [1] Cell Types: 786-O-HRE-Luc cell line Tested Concentrations: 0.003-20 μM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated no cytotoxicity to 786-O-Luc cells [1]. 786-O-Luc cells.
References	[1]. Insight into the binding mode of HIF-2 agonists through molecular dynamic simulations and biological validation. Eur J Med Chem. 2021 Feb 5;211:112999.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~240.33 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.01 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	2.4033 mL	12.0166 mL	24.0333 mL
	5 mM	0.4807 mL	2.4033 mL	4.8067 mL
	10 mM	0.2403 mL	1.2017 mL	2.4033 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.