Piriprost (potassium salt)
(Synonyms: U-60257B) 目录号 : GC16046
A novel 5-lipoxygenase inhibitor
Cas No.:88851-62-1
Sample solution is provided at 25 µL, 10mM.
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Piriprost (U 60257) is a leukotriene synthesis inhibitor [1].
Leukotrienes belong to a family of eicosanoid inflammatory mediators produced in leukocytes. Leukotrienes mainly act on a subfamily of G protein-coupled receptors. The production of leukotrienes is implicated in triggerring contractions in the smooth muscles lining the bronchioles and is a major cause of inflammation in asthma and allergic rhinitis [2].
Piriprost inhibited the formation of 5-hydroxyeicosatetraenoic acid (5-HETE), LTB4, and the sulfidopeptide leukotrienes with the IC50 values ranged from 9 to 14 μM for the mouse mast cells and 15-50 μM for the basophil leukemia cells. Piriprost weakly inhibited the solubilized LTC synthase of rat basophil leukemia cells with the IC50 of 1.5 mM [1]. Piriprost increased alkaline phosphatase (ALP) activity in cultured endometrial stromal cells. Piriprost (100 μM) inhibited 5-lipoxygenase activity and decreased 5-hydroxy-eicosatetraenoic acid (a 5-lipoxygenase product) by 53% [3].
In smoke-exposed rabbits, pretreatment with piriprost attenuated the smoke-induced increase in alveolar-capillary barrier permeability and decrease in plasminogen activator activity and causes a swelling of type I alveolar epithelium [4].
References:
[1] Bach M K, Brashler J R, White G J, et al. Experiments on the mode of action of piriprost (U-60,257), an inhibitor of leukotriene formation in cloned mouse mast cells and in rat basophil leukemia cells[J]. Biochemical pharmacology, 1987, 36(9): 1461-1466.
[2] Smith M J H, Ford‐Hutchinson A W, Bray M A. Leukotriene B: a potential mediator of inflammation[J]. Journal of Pharmacy and Pharmacology, 1980, 32(1): 517-518.
[3] Cejic S S, Kennedy T G. Examination of the effects of piriprost (U-60,257 B) on alkaline phosphatase activity of rat endometrial stromal cells in vitro[J]. Prostaglandins, 1991, 42(2): 179-189.
[4] itten M L, Grad R, Quan S F, et al. Piriprost pretreatment attenuates the smoke-induced increase in 99mTcDTPA lung clearance[J]. Experimental lung research, 1990, 16(4): 339-353.
| Cas No. | 88851-62-1 | SDF | |
| 别名 | U-60257B | ||
| 化学名 | 1,4(R),5(R),6-tetrahydro-5-hydroxy-4-[(1E,3S)-3-hydroxy-1-octenyl]-1-phenyl-cyclopenta[b]pyrrole-2-pentanoic acid, monopotassium salt | ||
| Canonical SMILES | CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC2=C1C=C(CCCCC([O-])=O)N2C3=CC=CC=C3.[K+] | ||
| 分子式 | C26H34NO4 • K | 分子量 | 463.7 |
| 溶解度 | ≤43mg/ml in ethanol;30mg/ml in DMSO;8.6mg/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。 |
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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 | 2.1566 mL | 10.7828 mL | 21.5657 mL |
| 5 mM | 0.4313 mL | 2.1566 mL | 4.3131 mL |
| 10 mM | 0.2157 mL | 1.0783 mL | 2.1566 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