Arginase inhibitor 1 ≥98%
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| 包装规格: | 5mg in glass bottle |
| 溶解性: | 溶于DMSO(≥48mg/mL)和H2O(≥30mg/mL) |
| 产品描述: | 基本信息 产品编号: A11588 产品名称: Arginase inhibitor 1 CAS: 1345808-25-4 储存条件 粉末 -20℃ 四年 分子式: C13H27BN2O4 溶于液体 -80℃ 六个月 分子量 286.18 -20℃ 一个月 化学名: (2R)-2-amino-6-borono-2-(2-piperidin-1-ylethyl)hexanoic acid Solubility (25°C): 体外: DMSO ≥48mg/mL(167.73mM) Ethanol Water ≥30mg/mL(104.83mM) 体内(现配现用): 1.请依序添加每种溶剂:PBS Solubility:65mg/mL(227.13mM);Clear solution; Need ultrasonic 2.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline,Solubility:≥1.67mg/mL(5.84mM);Clear solution 此⽅案可获得≥1.67mg/mL(5.84mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL16.699999mg/mL的澄清DMSO储备液加到400μLPEG300中,混合均匀;向上述体系中加⼊50μLTween-80,混合均匀;然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 3.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥1.67mg/mL(5.84mM);Clear solution 此⽅案可获得≥1.67mg/mL(5.84mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL16.699999mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中,混合均匀。 4.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥1.67mg/mL(5.84mM);Clear solution 此⽅案可获得≥1.67mg/mL(5.84mM,饱和度未知)的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例,取100μL16.699999mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。 <1mg/mL表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 3.4943mL 17.4715mL 34.9430mL 5mM 0.6989mL 3.4943mL 6.9886mL 10mM 0.3494mL 1.7472mL 3.4943mL 生物活性 产品描述 一种有效的人精氨酸酶(arginasesI和II)抑制剂。 靶点 IC50: 223nM (arginases I), 509nM (arginases II) 体外研究 Arginase inhibitor 1inhibits human arginases I and II with IC50s of 223±22.3 and 509±85.1nM, 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 IC50 for Arginase inhibitor 1 is 8μM in CHO Cells Over-Expressing hArgI 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 10mg/kg by bolus through a preimplanted cannula at a dosing volume of 1 mL/kg, and orally at 10mg/kg via gavage at a dosing volume of 2 mL/kg. Following i.v. dosing with 10mg/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 (10mg/kg, p.o.) is 28% with a Cmax of 0.45mg/L 推荐实验方法(仅供参考) Animal Administration Rats Single dose pharmacokinetics are evaluated in male Sprague-Dawley rats by intravenous bolus (i.v.) and oral (p.o.) dosing. Three rats are evaluated per dose group. Arginase inhibitor 1 is freshly formulated in 0.9% saline prior to dosing, at 10mg/mL for i.v. dosing at a dose volume of 1mL/kg animal body weight, and at 5mg/mL for p.o. dosing at a dose volume of 2mL/kg. Animals are fasted overnight prior to dosing, with water given ad libitum. Arginase inhibitor 1 is administered i.v. through a preimplanted cannula or orally by gavage. Food is reintroduced to animals 4 h following dosing. Blood samples are collected through preimplanted cannulae (dual cannulated animals used for i.v. dosing; blood collection separate from dosing cannula) at 0.25mL per draw, followed by volume replacement with 0.9% saline. Samples are collected at predose 0.083 (i.v. only), 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h following dosing. Blood samples are maintained on ice and centrifuged at 10 000g to obtain plasma. Plasma is frozen at -20 °C prior to analysis. Analysis is performed by LC/MS/MS. Pharmacokinetic evaluation is performed using standard noncompartmental analyses in Phoenix WinNonlin software |
| 保存条件: | -20℃ |
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