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 2 篇同行评审文献引用。
概述
Domperidone 是一种多巴胺受体抑制剂，是一种抗多巴胺试剂。A peripheral D2DR inhibitor.
Information
Domperidone is an oraldopamine D2 receptorantagonist, used to treat nausea and vomiting.
In vitro
Domperidone (a D2R antagonist) inhibits Equilibrative NT1 (ENT1) activity more in the presence than in the absence of Bromocriptine and displays an IC50 value lower than that of Bromocriptine or Ergovaline in Madin-Darby bovine kidney (MDBK) cells.
In vivo
Domperidone (0.1 mg/kg) results in a significant decrease in feeding behavior and stimulation of basal metabolism, but has no effect on locomotor activity of rats in a Phenomaster system. Domperidone (1.1 mg/kg and 5.5 mg/kg, oral) significantly increases laminar microvascular blood flow (LMBF) in horses, compared with baseline values, beginning 4 hours after administration, and this effect persisted for at least 8 hours. Domperidone (0.2 mg/kg, i.v.) significantly increases laminar microvascular blood flow (LMBF) in horses, compared with baseline values, at 10 and 12 hours after administration. Domperidone can ameliorate deleterious reproductive effects and reduce weight gain associated with fescue toxicosis in heifers. Domperidone-treated mares have shorter gestation duration and foaled closer to their expected parturition date than did control mares. Domperidone-treated mares have higher Mammary gland scores and serum prolactin concentration. Domperidone (5 mg/kg, oral) increases peak plasma acetaminophen concentration and area under the curve in rats, indicating increased gastric emptying. Domperidone decreases the dopamine-induced contractile activity of midjejunal longitudinal muscle strips in rats.
Cell Data
cell lines：SET-2 and TEL-JAK Ba/F3 cells
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
英文别名
5-chloro-1-[1-[3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Domperidone
生化机理
多潘立酮是一种口服多巴胺 D2 受体拮抗剂，用于治疗恶心和呕吐。
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
多巴胺 D2 受体拮抗剂
名称和识别符
EC号
260-968-7
分子类型
小分子
Isomeric SMILES
C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O
分子量
425.91
Reaxy-Rn
903774
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=903774&ln=
技术文档
高级数据
产品属性
| ALogP | 3.9 |
|---|
关联靶点（人）
DRD2
Tclin
D（2）多巴胺受体(D(2) dopamine receptor)
(4 活性数据)
DRD3
Tclin
D(3) 多巴胺受体(D(3) dopamine receptor)
(5 活性数据)
HTR2A
Tclin
5-羟色胺受体 2A(5-hydroxytryptamine receptor 2A)
(2 活性数据)
KCNH2
Tclin
钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2)
(6 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro 5%TFA 3.06 mg/mL (17.37 mM); DMSO: 0.1 mg/mL (0.56 mM); Water: Insoluble;
熔点
243°C
安全和危险性（GHS）
信号词
警告
危险声明
H361: 怀疑破坏生育力或未出生的孩子
WGK Germany
3
RTECS
DE2275900
Merck Index
3418
个人防护装备
Eyeshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges
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:
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）