计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，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 1 篇同行评审文献引用。
概述
Desloratadine is a potent and selective histamine H1-receptor agonist with a half life of 21-24 hours. Experiments sμggest that this compound also exerts antioxidant effects in vitro. Other studies show that H1-receptor binding by desloratadine is reversible and that, over time, desloratadine dissociates from membrane H1-recepters. Desloratadine has also demonstrated the ability to block ICAM-1 upregulation and NFκB activation in primary bronchial and transformed respiratory epithelial cells in vitro.Desloratadine是人H1受体拮抗剂。
Information
Desloratadine (SCH-34117, NSC 675447) is a potent antagonist for humanhistamine H1receptor withIC50of 51 nM.
In vitro
Desloratadine is a competitive antagonist of carbachol-induced contractions in isolated rabbit iris smooth muscle with pA2 of 6.67. Desloratadine binds to the human H1 receptor with Ki value of 0.87 nM in displacing tritiated mepyramine. Desloratadine (100 nM to 10 μM) inhibits both IgE-mediated and non–IgE-mediated generation of the cytokines IL-4 and IL-13 by human basophils. Desloratadine (300 nM to 100 μM) inhibits both IgE and non–IgE-mediated histamine release from human peripheral blood basophils. Desloratadine (0.1 μM to 10 μM) is also shown to inhibit platelet-activating factor-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion in eosinophils obtained from patients with allergic rhinitis or allergic asthma. Desloratadine (1 μM-10 μM) dose-dependently inhibits the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μM-10 μM) dose-dependently inhibits IL-13 secretion from basophils activated with IL-3 and PMA from human basophils. Desloratadine (10 μM) pretreatment results in a substantial decrease of the induced cytokine message in cultured basophils. Desloratadine (10 μM) pretreatment causes approximately an 80% reduction in the IL-4 message accumulated with anti-IgE activation in cultured basophils. Desloratadine (10 μM) also inhibits the histamine and IL-4 protein secreted into the supernatants of cultured basophils. [3H]Desloratadine binds to the human histamine H1 receptor expressed in CHO cells with Kd of 1.1 nM. Desloratadine is 52, 57, 194, and 153 times more potent than cetirizine, ebastine, fexofenadine, and loratadine, respectively, in competition-binding studies.
In vivo
Desloratadine (1 mg/mL, 3 mg/mL and 10 mg/mL) induces a dose-dependent and long lasting mydriasis in the guinea-pig in vivo. Desloratadine inhibits histamine-induced paw edema with ED50 of 0.15 mg/kg in mice. Desloratadine inhibits an increase in microvascular permeability in response to a histamine challenge to the upper airway of guinea pigs with ED50 of 0.9 μg. Desloratadine (5 mg/kg) causes inhibition of oxotremorine-induced tremor by disrupting blood-brain barrier in conscious mice. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
SCH-34117, NSC 675447 | 5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Desloratadine
生化机理
地氯雷他定（SCH-34117，NSC 675447）是一种强效的人类组胺 H1 受体拮抗剂，IC50 为 51 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
组胺 H1 受体拮抗剂
名称和识别符
EC号
638-878-8
分子类型
小分子
Isomeric SMILES
C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
分子量
310.83
Reaxy-Rn
4263164
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4263164&ln=
技术文档
高级数据
产品属性
| ALogP | 4.5 |
|---|
关联靶点（人）
HRH1
Tclin
组胺 H1 受体(Histamine H1 receptor)
(7 活性数据)
SLC6A4
Tclin
钠依赖性血清素转运体(Sodium-dependent serotonin transporter)
(2 活性数据)
CHRM3
Tclin
毒蕈碱乙酰胆碱受体 M3(Muscarinic acetylcholine receptor M3)
(1 活性数据)
CHRM4
Tclin
毒蕈碱乙酰胆碱受体 M4(Muscarinic acetylcholine receptor M4)
(1 活性数据)
CHRM2
Tclin
毒蕈碱乙酰胆碱受体 M2(Muscarinic acetylcholine receptor M2)
(1 活性数据)
HTR2A
Tclin
5-羟色胺受体 2A(5-hydroxytryptamine receptor 2A)
(2 活性数据)
CHRM1
Tclin
毒蕈碱乙酰胆碱受体 M1(Muscarinic acetylcholine receptor M1)
(1 活性数据)
HTR2C
Tclin
5-羟色胺受体 2C(5-hydroxytryptamine receptor 2C)
(2 活性数据)
HTR2B
Tclin
5-羟色胺受体 2B(5-hydroxytryptamine receptor 2B)
(2 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 18 mg/mL (61.15 mM); Ethanol: 3 mg/mL (10.19 mM); Water: Insoluble;
熔点
157 °C
安全和危险性（GHS）
信号词
危险
危险声明
H302: 吞食有害
H318: 造成严重的眼睛损伤
H361: 怀疑破坏生育力或未出生的孩子
H411: 对水生生物有毒并具有长期持续影响
Merck Index
2922
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:
技术文档和文章
此产品的引用文献
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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危险品化学品经营许可证（带存储）