Fuzapladib (IS-741) sodium is an orally bioactive leukocyte function-associated antigen type 1 (LFA-1) activation inhibitor, a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts its anti-inflammatory effects by inhibiting the migration of white blood cells to sites of inflammation.

Physicochemical Properties

Molecular Formula	C15H20F3N3NAO3S
Molecular Weight	402.39
Exact Mass	401.1
CAS #	141284-73-3
Related CAS #	Fuzapladib;141283-87-6
PubChem CID	23711649
Appearance	Off-white to light yellow solid powder
Boiling Point	522.9ºC at 760mmHg
Flash Point	270.1ºC
Vapour Pressure	9.19E-12mmHg at 25°C
LogP	5.127
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	5
Heavy Atom Count	26
Complexity	563
Defined Atom Stereocenter Count	0
InChi Key	RVWHCCQDZKMPAZ-UHFFFAOYSA-M
InChi Code	InChI=1S/C15H20F3N3O3S.Na/c1-2-25(23,24)21-13-12(8-11(9-19-13)15(16,17)18)20-14(22)10-6-4-3-5-7-10;/h8-10H,2-7H2,1H3,(H2,19,20,21,22);/q;+1/p-1
Chemical Name	sodium;[3-(cyclohexanecarbonylamino)-5-(trifluoromethyl)pyridin-2-yl]-ethylsulfonylazanide
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	Fuzapladib sodium (IS-741 sodium) at 1 μM for three hours can effectively prevent HL-60 cells from adhering to HUVEC when they are stimulated with lipopolysaccharide [3].
ln Vivo	Fuzapladib sodium (IS-741 sodium) (po, 50 mg/kg, 7 days) effectively reduces trinitrobenzene sulfonic acid (TNBS) ileitis in rats by inhibiting neutrophil recruitment into inflammatory lesions [4].
Animal Protocol	Animal/Disease Models: Rats[2] Doses: 50 mg/kg Route of Administration: Po; for 7 days Experimental Results: Dramatically diminished myeloperoxidase (MPO) activity and mucosal IL- 8 levels in rat ileum, diminished polymorphonuclear cells and Mac-1 positivity Infiltration of cells into inflammatory lesions, effectively alleviated trinitrobenzenesulfonic acid (TNBS)-induced ileitis.
References	[1]. Fuzapladib reduces postsurgical inflammation in the intestinal muscularis externa. J Vet Med Sci. 2023 Sep 21. [2]. C Bassi. IS-741 (Ishihara Sangyo). Curr Opin Investig Drugs. 2001 Apr;2(4):510-2. [3]. Effect of IS-741 on cell adhesion between human umbilical vein endothelial cells and HL-60 cells. Biol Pharm Bull. 1999 Feb;22(2):127-31. [4]. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9.
Additional Infomation	See also: Fuzapladib (has active moiety).

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (248.52 mM

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.21 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 (6.21 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 (6.21 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	2.4852 mL	12.4258 mL	24.8515 mL
	5 mM	0.4970 mL	2.4852 mL	4.9703 mL
	10 mM	0.2485 mL	1.2426 mL	2.4852 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.