BayCysLT2
(Synonyms: CAY10633) 目录号 : GC13020A potent CysLT2 receptor antagonist
Cas No.:712313-33-2
Sample solution is provided at 25 µL, 10mM.
BayCysLT2, an isophthalic acid derivative, is a selective and potent CysLT2 receptor antagonist [1].
Cysteinyl leukotrienes (CysLTs) belong to a family of G protein-coupled receptors (GPCRs). The cysteinyl leukotrienes (CysLTs) are inflammatory mediators associated with neuronal injury after brain ischemia through the activation of their receptors, CysLT1R and CysLT2R [2].
In vitro: BayCysLT2 inhibited radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively [1]. BayCysLT2 reversed LTC4-stimulated perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts in a concentration-dependent manner [1]. BayCysLT2 protected astrocytes from ischemic injury [3].
In vivo: BayCysLT2 attenuated myocardial infarction damage but also inhibited LTD4-induced Evans blue dye leakage in the mouse ear vasculature [4].
References:
[1] M. Harter, J. Erguden, F. Wunder, et al. Isophtalic acid derivatives. 10/537,623, 1-104 (2006).
[2] Takasaki J, Kamohara M, Matsumoto M, et al. The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT 2 receptor[J]. Biochemical and biophysical research communications, 2000, 274(2): 316-322.
[3] X. J. Huang, W.P. Zhang, C.T. Li, W.Z. Shi, S.H. Fang, Y.B. Lu, Z. Chen, E.Q. Wei. Activation of CysLT receptors induces astrocyte proliferation and death after oxygen–glucose deprivation. Glia, 56 (2008), pp. 27–37
[4] N. C. Ni, D. Yan, L.L. Ballantyne, A. Barajas-Espinosa St, T. Amand, D.A. Pratt, C.D. Funk. A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice. J. Pharmacol. Exp. Ther., 339 (2011), pp. 768–778
Cas No. | 712313-33-2 | SDF | |
别名 | CAY10633 | ||
化学名 | 3-[[(3-carboxycyclohexyl)amino]carbonyl]-4-[3-[4-(4-phenoxybutoxy)phenyl]propoxy]-benzoic acid | ||
Canonical SMILES | O=C(NC1CCCC(C(O)=O)C1)C2=CC(C(O)=O)=CC=C2OCCCC(C=C3)=CC=C3OCCCCOC4=CC=CC=C4 | ||
分子式 | C34H39NO8 | 分子量 | 589.7 |
溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | 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。 |
||
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 | 1.6958 mL | 8.4789 mL | 16.9578 mL |
5 mM | 0.3392 mL | 1.6958 mL | 3.3916 mL |
10 mM | 0.1696 mL | 0.8479 mL | 1.6958 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet