| Identification | Back Directory | [Name]
Arginase inhibitor 1 | [CAS]
1345808-25-4 | [Synonyms]
Arginase inhibitor 1
1-Piperidinebutanoic acid, α-amino-α-(4-boronobutyl)-, (αR)-
(alphaR)-alpha-Amino-alpha-(4-boronobutyl)-1-piperidinebutanoic acid | [Molecular Formula]
C13H27BN2O4 | [MDL Number]
MFCD28167713 | [MOL File]
1345808-25-4.mol | [Molecular Weight]
286.18 |
| Chemical Properties | Back Directory | [Boiling point ]
523.0±60.0 °C(Predicted) | [density ]
1.147±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | [solubility ]
DMSO: 50 mg/ml; Water: 30 mg/ml | [form ]
Powder | [pka]
2.22±0.44(Predicted) | [color ]
White to gray |
| Hazard Information | Back Directory | [Description]
Arginase inhibitor 1 is an inhibitor of arginase I and II (IC50s = 223 and 509 nM, respectively, for the recombinant human enzymes). It decreases arginase I activity in CHOK cells expressing human arginase I (IC50 = 8 μM). Arginase inhibitor 1 (100 mg/kg, i.v.) reduces infarct size in a rat model of myocardial ischemia and reperfusion injury induced by left-main coronary artery occlusion. | [Uses]
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively. | [in vivo]
Following i.v. dosing with 10 mg/kg in fasted animals, Arginase inhibitor 1has a terminal elimination half-life (t1/2) of 3.3 h with a volume of distribution and total body clearance of 1.86 L/kg and 7.89 mL/min/kg, respectively. The oral bioavailability of Arginase inhibitor 1 (10 mg/kg, p.o.) is 28% with a Cmax of 0.45 mg/L[1]. | [References]
[1] 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. DOI:10.1021/jm400014c |
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