BI-9627
目录号 : GC34492An NHE1 inhibitor
Cas No.:1204329-34-9
Sample solution is provided at 25 µL, 10mM.
BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1), with IC50 values of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively.1 It is greater than 30-fold selective for NHE1 over NHE2 and is inactive at NHE3 up to 16 μM in a pHi assay. BI-9627 inhibits phenylephrine-induced hypertrophy in neonatal rat cardiomyocytes.2 It increases recovery of left ventricular developed pressure and inhibits increases in left ventricular end-diastolic pressure (LVEDP) in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury when used at a concentration of 100 nM.1 BI-9627 (45 and 150 ppm in the diet) also attenuates decreases in left ventricular end-systolic pressure and increases in LVEDP in coronary artery-ligated rats.2
1.Huber, J.D., Bentzien, J., Boyer, S.J., et al.Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the ratJ. Med. Chem.55(16)7114-7140(2012) 2.Kili?, A., Huang, C.X., Rajapurohitam, V., et al.Early and transient sodium-hydrogen exchanger isoform 1 inhibition attenuates subsequent cardiac hypertrophy and heart failure following coronary artery ligationJ. Pharmacol. Exp. Ther.351(3)492-499(2014)
Cas No. | 1204329-34-9 | SDF | |
Canonical SMILES | NC(NC(C1=CC=C(C2CCN(C(C)=O)CC2)C(C(F)(F)F)=C1)=O)=N | ||
分子式 | C16H19F3N4O2 | 分子量 | 356.34 |
溶解度 | DMF: 10mg/mL,DMSO: 20mg/mL,DMSO:PBS (pH 7.2) (1:7): 0.12mg/mL | 储存条件 | Store at -20°C |
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.8063 mL | 14.0315 mL | 28.0631 mL |
5 mM | 0.5613 mL | 2.8063 mL | 5.6126 mL |
10 mM | 0.2806 mL | 1.4032 mL | 2.8063 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
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