货号:A108288 同义名: 普仑司特 / ONO-1078;ONO-RS-411
Pranlukast 是一种选择性的 CysLT1 受体拮抗剂,对 CysLT1 受体具有高亲和力,IC50 值为 0.5 nM。Pranlukast 具有抗过敏和抗哮喘作用,可用于过敏性疾病和哮喘的研究。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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产品名称 | LTR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Montelukast Sodium | ✔ | 98% | |||||||||||||||||
MK571 | ✔ | 98% | |||||||||||||||||
Zafirlukast | ✔ | 99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Pranlukast is a selective, competitive antagonist of the cysteinyl leukotrienes, leukotriene (LT) C4, LTD4 and LTE4, antagonising binding at the cysteinyl leukotriene type 1 (CysLT1) receptor. In isolated human bronchial smooth muscle preparations, pranlukast caused a concentrationdependent inhibition or reversal of LTC4-, LTD4- and house dust antigen-induced bronchial contraction, but had minimal or no effect on histamine (H)- prostaglandin F2α-, acetylcholine- or thromboxane, A2 (TXA2) mimetic agonist-induced contraction (at 37°C)[3]. In vitro , antigen-induced contraction was inhibited more effectively with pranlukast than with an H1-receptor antagonist; however, pranlukast in combination with an H1-receptor antagonist was more potent than either agent alone[4].Pranlukast has shown a range of anti-inflammatory effects on airways in animal models, including attenuation or inhibition of microvascular leakage in the trachea, bronchi and small airways,LTD4-, capsaicin- or allergen-induced eosinophilia in bronchoalveolar lavage fluid (BAL), bronchial epithelial and subepithelial tissue or lung parenchyma and the expression of mRNA for interleukin-5 in BAL cells[5]. In addition, pranlukast inhibited airway smooth muscle DNA synthesis and reduced allergen-induced airway smooth muscle cell thickness in repeatedly ovalbumin-sensitised rats[6].Animal models show that pranlukast is cleared through metabolic transformation (primarily glucuronic acid conjugation); an in vitro study indicated that the drug is metabolised via cytochrome P450 (CYP) enzymes. The main metabolites formed are mono- and dihydroxylated molecules and their glucuronide conjugates[7]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00127647 | Rhinitis, Allergic, Seasonal | Phase 3 | Completed | - | - |
NCT01539304 | Perennial Allergic Rhinitis | Phase 3 | Completed | - | Korea, Republic of ... 展开 >> Seoul National University Hodpital Seoul, Korea, Republic of 收起 << |
NCT00410735 | Chronic Sinusitis | Phase 3 | Completed | - | Japan ... 展开 >> Chubu region Chubu, Japan Hokuriku region Hokuriku, Japan Kanto region Kanto, Japan Kinki region Kinki, Japan Kyushu region Kyushu, Japan Tohoku region Tohoku, Japan 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.38mL 2.08mL 1.04mL |
20.77mL 4.15mL 2.08mL |
CAS号 | 103177-37-3 |
分子式 | C27H23N5O4 |
分子量 | 481.503 |
别名 | 普仑司特 ;ONO-1078;ONO-RS-411;SB 205312 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 35 mg/mL(72.69 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |