LY171883
(Synonyms: 油酸三乙醇胺) 目录号 : GC13087
Selective, potent LTD4 receptor antagonist
Cas No.:88107-10-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
LY171883 is a leukotriene D4 receptor antagonist.
Leukotriene D4 is one of the leukotrienes, whose major function is to induce the smooth muscle contraction, leading to vasoconstriction and bronchoconstriction. Leukotriene D4 can also increase vascular permeability.
In vitro: In GH(3) cells, LY-171883 was able to reversibly increase the amplitude of Ca(2+)-activated K(+) current concentration-dependently with an EC(50) value of 15 μM. Moreover, the treatment of LY-171883 to cytosolic face did not affect single channel conductance of large-conductance Ca(2+)-activated K(+) channels in excised inside-out patches recorded from GH(3) cells, however, LY-171883 did increase the channel activity. In addition, the LY-171883-stimulated activity of BK(Ca) channels was dependent on membrane potential [1].
In vivo: The effect of LY-171883 on the respiratory and cardiovascular changes in endotoxemia was studied in unanesthetized sheep. In group one, LY-171883 at 4 mg/kg was i.v. injected. In group two, Escherichia coli endotoxin (1 μg/kg) was infused, and in group three, LY-171883 at 4 mg/kg was administered before and after the same dose of endotoxin. Results showed that infusion of LY-171883 in group one did not alter baseline ventilatory and cardiovascular measurements. In group two, a two-phase pulmonary response was found. An early pulmonary hypertension phase with a fall in cardiac index was observed in group three [2].
Clinical trial: Up to now, no clinical data have been released.
References:
[1] PC Li et al. Enhanced Activity of Ca2+-Activated K+ Channels by 1-[2-Hydroxy-3-Propyl-4-[(1h-Tetrazol-5-Yl)butoxyl]phenyl] Ethanone (LY-171883) in Neuroendocrine and Neuroblastoma Cell Lines. J Cell Physiol 192 (2), 188-199. 8 2002.
[2] Gross D, Ben Dahan J, Landau EH, Krausz MM. Effect of leukotriene inhibitor LY-171883 on the pulmonary response to Escherichia coli endotoxemia. Crit Care Med. 1990 Feb;18(2):190-7.
| Cas No. | 88107-10-2 | SDF | |
| 别名 | 油酸三乙醇胺 | ||
| 化学名 | 1-[2-hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]-ethanone | ||
| Canonical SMILES | CCCc1c(OCCCCc2nnn[nH]2)ccc(C(=O)C)c1O | ||
| 分子式 | C16H22N4O3 | 分子量 | 318.4 |
| 溶解度 | ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide | 储存条件 | Room temperature |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1407 mL | 15.7035 mL | 31.407 mL |
| 5 mM | 0.6281 mL | 3.1407 mL | 6.2814 mL |
| 10 mM | 0.3141 mL | 1.5704 mL | 3.1407 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。