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中文名称: Arginase inhibitor 1
英文名称: Arginase inhibitor 1
CAS No: 1345808-25-4
分子式: C13H27BN2O4
分子量: 286.18
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
A11588 Arginase inhibitor 1 ≥98% (psaitong)
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℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
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