HAMI3379
目录号 : GC17092A potent CysLT2 receptor antagonist
Cas No.:1245653-57-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 37.9 nM: blocks radioligand binding of leukotriene D4 (LTD4) to cysteinyl leukotriene 2 (CysLT2).
IC50: 3.8 nM: antagonizes LTD4-induced intracellular calcium mobilization in a CysLT2 receptor reporter cell line.
IC50: 4.4 nM: antagonizes leukotriene C4 (LTC4) -induced intracellular calcium mobilization in a CysLT2 receptor reporter cell line.
HAMI3379, as a potent CysLT2 receptor antagonist, blocks radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines. In a CysLT2 receptor reporter cell line, HAMI3379 antagonizes LTD4- and LTC4-induced intracellular calcium mobilization. In contrast, HAMI3379 exhibits very low potency on a CysLT1 receptor reporter cell line. Additionally, HAMI3379 does not exhibit any agonistic activity on both CysLT2 and CysLT1 receptor cell lines. CysLTs LTC4 and LTD4 are potent mediators of hypersensitivity and asthma reactions. They increase the permeability of microvascular, elicit bronchoconstriction, functioning as vasoconstrictors of coronary arteries, which are transduced by CysLT1 and CysLT2.
In vitro: In a murine microglial cell line (BV-2 cells), HAMI3379 effectively dampened lipopolysaccharide (LPS) -induced phagocytosis. In addition, HAMI3379 dose-dependently decreased the LPS-induced overproduction of proinflammatory cytokines which included tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 [1].
In vivo: Male Sprague–Dawley rats were injected intraperitoneally with HAMI 3379 at a dose of 0.1 mg/kg at 0, 1, 2 and 4 h. After 24 h, HAMI 3379 attenuated the acute brain injury after middle cerebral artery occlusion (MCAO). In addition, HAMI 3379 weakened the neurological deficits and decreased brain edema, infarct volume, and neuronal loss and degeneration after MACO. Moreover, HAMI 3379 blocked the release of interferon-γ, cytokines IL-1β, and TNF-α into the cerebrospinal fluid and serum after MACO [2].
References:
[1]. Chen, L., Yang, Y., Li, C., Zhang, S., Zheng, W., Wei, E., & Zhang, L. CysLT2 receptor mediates lipopolysaccharide-induced microglial inflammation and consequent neurotoxicity in vitro. Brain Research. 2015; 1624: 433-445.
[2]. Shi, Q., Wang, H., Liu, Z., Fang, S., Song, X., & Lu, Y. et al. HAMI 3379, a CysLT2R antagonist, dose- and time-dependently attenuates brain injury and inhibits microglial inflammation after focal cerebral ischemia in rats. Neuroscience. 2015; 291: 53-69.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6787 mL | 8.3935 mL | 16.787 mL |
| 5 mM | 0.3357 mL | 1.6787 mL | 3.3574 mL |
| 10 mM | 0.1679 mL | 0.8393 mL | 1.6787 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 | ||||||||||
计算结果:
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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