(ALPHAR)-ALPHA-氨基-ALPHA-(4-硼酸基丁基)-1-哌啶丁酸
- CAS号:1345808-25-4
- 英文名:Arginase inhibitor 1
- 中文名:(ALPHAR)-ALPHA-氨基-ALPHA-(4-硼酸基丁基)-1-哌啶丁酸
- CBNumber:CB52677054
- 分子式:C13H27BN2O4
- 分子量:286.18
- MOL File:1345808-25-4.mol
- 沸点 :523.0±60.0 °C(Predicted)
- 密度 :1.147±0.06 g/cm3(Predicted)
- 储存条件 :Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- 溶解度 :DMSO: 50 mg/ml; Water: 30 mg/ml
- 形态 :Powder
- 酸度系数(pKa) :2.22±0.44(Predicted)
- 颜色 :White to gray
(ALPHAR)-ALPHA-氨基-ALPHA-(4-硼酸基丁基)-1-哌啶丁酸性质、用途与生产工艺
- 生物活性 Arginase inhibitor 1 是一种有效的人精氨酸酶 (arginases I 和 II)抑制剂,IC50 分别为 223 和 509 nM。
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靶点
IC50: 223 nM (arginases I), 509 nM (arginases II)
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体外研究
Arginase inhibitor 1inhibits human arginases I and II with IC 50 s of 223±22.3 and 509±85.1 nM, respectively, and is active in a recombinant cellular assay overexpressing human arginase I (CHO cells). Arginase inhibitor 1 is a novel second generation 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 IC 50 for Arginase inhibitor 1 is 8 μM in CHO Cells Over-Expressing hArgI.
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体内研究
A 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 preimplanted 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 (t 1/2 ) 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 C max of 0.45 mg/L.
- 更新日期:2024/11/08
- 产品编号:HY-15775
- 产品名称:(ALPHAR)-ALPHA-氨基-ALPHA-(4-硼酸基丁基)-1-哌啶丁酸 Arginase inhibitor 1
- CAS编号:1345808-25-4
- 包装:2mg
- 价格:1600元
- 更新日期:2024/11/08
- 产品编号:HY-15775
- 产品名称:(ALPHAR)-ALPHA-氨基-ALPHA-(4-硼酸基丁基)-1-哌啶丁酸 Arginase inhibitor 1
- CAS编号:1345808-25-4
- 包装:5mg
- 价格:2400元
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