Arginase 1, Inhibitor

Arginase inhibitor 1

Cat. Num. AAA5752716

• Purity: 98.00%
• Synonyms: Arginase 1; Arginase inhibitor 1; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 48mg/mL (167.73mM); H2O: 30mg/mL (104.83mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C13H27BN2O4
• SMILES: O=C(O)[C@@](CCN1CCCCC1)(N)CCCCB(O)O
• CAS Number: 1345808-25-4
• Target & IC50: arginases I: ic50 223nM; arginases II: ic50 509nM
• In Vitro: Pharmacokinetic evaluation of Arginase inhibitor 1 is conducted after intravenous (i.v.) and oral (p.o.) dosing in male Sprague-Dawley rats (n=3 per dose route). Arginase inhibitor 1 is formulated in 0.9% saline and administered intravenously at 10mg/kg by bolus through a pre-implanted cannula at a dosing volume of 1mL/kg, and orally at 10mg/kg via gavage at a dosing volume of 2mL/kg. Following i.v. dosing with 10mg/kg in fasted animals, Arginase inhibitor 1has a terminal elimination half-life (t1/2) of 3.3 hours with a volume of distribution and total body clearance of 1.86L/kg and 7.89mL/min/kg, respectively. The oral bioavailability of Arginase inhibitor 1 (10mg/kg, p.o.) is 28% with a Cmax of 0.45mg/L.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for Arginase 1, inhibitor

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II (IC50s: 223 and 509nM).

References

Van Zandt MC, et al. Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potentinhibitors of human arginases I and II for treatment,of myocardial reperfusion injury. J Med Chem. 2013 Mar 28;56(6):2568-80.
Van Zandt MC, et al. Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potentinhibitors of human arginases I and II for treatment,of myocardial reperfusion injury. J Med Chem. 2013 Mar 28;56(6):2568-80.