计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Rupatadine (UR-12592) Fumarate 是一种有效的，具有口服活性的长效 PAF/H1 受体的双抑制剂，Ki 值分别为 0.55 μM 和 0.1 μM。Rupatadine Fumarate 可用于过敏性鼻炎和荨麻疹的研究。
Information
Rupatadine is an inhibitor ofPAFRandhistamine (H1) receptorwithKiof 550 nM and 102 nM, respectively.
In vitro
Rupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29 ± 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4(LTD4). It also competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2= 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation. In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α.
In vivo
Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 μg/kg i.v.). Moreover, it potently inhibits PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.). Rupatadine\'s duration of action is long, as assessed by the histamine- and PAF-induced increase in vascular permeability test in dogs (42 and 34% inhibition at 26 h after 1 mg/kg p.o.). Rupatadine at a dose of 100 mg/kg p.o. neither modifies spontaneous motor activity nor prolongs barbiturate-sleeping time in mice, which indicates a lack of sedative effects.
Cell Data
cell lines：
Concentrations：up to 100 μM
Incubation Time：5 mins
Powder Purity:≥99%
规格
英文别名
5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-, (2E)-2-butenedioate (1:1)
规格或纯度
10mM in DMSO
英文名称
Rupatadine Fumarate
生化机理
鲁帕他定是 PAFR 和组胺（H1）受体的抑制剂，其Ki值分别为 550 nM 和 102 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
642-920-0
分子类型
小分子
Isomeric SMILES
CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2.C(=C/C(=O)O)\C(=O)O
PubChem CID
分子量
532.03
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 29 mg/mL (98.5 mM); Ethanol: 29 mg/mL (98.5 mM); Water: Insoluble;
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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