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Arginase inhibitor 1 is a potent inhibitor of human arginases I and II (IC50s: 223 and 509 nM).
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II (IC50s: 223 and 509 nM).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,670 | 35日内发货 | |
5 mg | ¥ 11,900 | 35日内发货 |
产品描述 | Arginase inhibitor 1 is a potent inhibitor of human arginases I and II (IC50s: 223 and 509 nM). |
靶点活性 | Arginases I:223 nM , Arginases II:509 nM |
体外活性 | Arginase inhibitor 1 is an arginase inhibitor with significant activity in a rat model of myocardial ischemia/reperfusion injury (MI/RI). Arginase inhibitor 1 is potent against hARG I in both in vitro enzyme and cellular assays. The IC50 for Arginase inhibitor 1 is 8 μM in CHO Cells Over-Expressing hArgI |
体内活性 | 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 10 mg/kg by bolus through a pre-implanted cannula at a dosing volume of 1 mL/kg, and orally at 10 mg/kg via gavage at a dosing volume of 2 mL/kg. 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. |
分子量 | 286.18 |
分子式 | C13H27BN2O4 |
CAS No. | 1345808-25-4 |
密度 | 1.147 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 30 mg/mL (104.83 mM) DMSO: 48 mg/mL (167.73 mM) | |||||||||||||||||||||||||||||||||||
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