BIZ 114 (Example 11) is a fatty acid analogue that effectively inhibits the NF-κΒ pathway activated by TNF-α. BIZ 114 may be utilized in the research/study of ophthalmic diseases like retinal degenerative diseases and ocular inflammatory diseases.

Physicochemical Properties

Molecular Formula	C24H40O3
Molecular Weight	376.57260799408
Exact Mass	376.297
CAS #	2099120-74-6
PubChem CID	129209358
Appearance	Colorless to light yellow liquid（Density：0.94 g/cm3）
LogP	7.5
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	18
Heavy Atom Count	27
Complexity	447
Defined Atom Stereocenter Count	0
SMILES	CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCCOC(CC)C(=O)O
InChi Key	JJBSGIKIKLMNBG-GKFVBPDJSA-N
InChi Code	InChI=1S/C24H40O3/c1-3-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-21-22-27-23(4-2)24(25)26/h8-9,11-12,14-15,17-18,23H,3-7,10,13,16,19-22H2,1-2H3,(H,25,26)/b9-8-,12-11-,15-14-,18-17-
Chemical Name	2-[(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoxy]butanoic acid
Synonyms	BIZ-114; BIZ114
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

Polyunsaturated fatty acids and their metabolites have a variety of significant biological functions because they are involved in numerous physiological and pathological processes. They have an impact on lipid metabolism and plasma lipids. They are integrated into the membranes of cells, where they affect many cell processes. In addition to controlling and influencing gene expression, they are also implicated in inflammatory disorders. The potential treatment and/or prevention of ophthalmic problems, specifically retinal disorders such diabetic retinopathy and age-related macular degeneration, as well as ocular inflammatory diseases, lies in the fatty acid derivatives[1].

References

[1]. Anne Kristin Holmeide. pid compounds and compositions and their opthalmic use. WO2017093732A1.

Solubility Data

Solubility (In Vitro)

DMSO : ~250 mg/mL (~663.89 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.33 mg/mL (6.19 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 23.3 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: ≥ 2.33 mg/mL (6.19 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 23.3 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	2.6555 mL	13.2777 mL	26.5555 mL
	5 mM	0.5311 mL	2.6555 mL	5.3111 mL
	10 mM	0.2656 mL	1.3278 mL	2.6555 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.