| CAS NO: | 88851-62-1 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 463.7 |
| Cas No. | 88851-62-1 |
| Formula | C26H34NO4·K |
| Synonyms | U-60257B |
| Solubility | ≤43mg/ml in ethanol;30mg/ml in DMSO;8.6mg/ml in dimethyl formamide |
| Chemical Name | 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+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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