Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
50mg |
|
||
Other Sizes |
|
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]. Noriyuki Kaji, et al. 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]. Shikama H, et al. 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]. Tetsuya Fukunaga, et al. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9. |
Molecular Formula |
C15H20F3N3NAO3S
|
---|---|
Molecular Weight |
402.39
|
CAS # |
141284-73-3
|
Related CAS # |
Fuzapladib;141283-87-6
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
[Na+].CCS([N-]C1N=CC(C(F)(F)F)=CC=1NC(C1CCCCC1)=O)(=O)=O
|
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)
|
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. View More
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. |
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.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.