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
概述
Aprepitant是一种有效的，选择性的神经激肽-1受体拮抗剂
Information
Aprepitant (MK-0869, L-754030) is a potent and selectiveneurokinin-1 receptorantagonist withIC50of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines includingG-CSF,IL-6,IL-8andTNFα. Aprepitant inhibitsHIVinfection of human macrophages.
In vitro
Aprepitant antagonizes the effects of substance P by binding to NK-1 receptors primarily in the CNS, but also in the periphery. Aprepitant, at concentrations of 0.1 nM displaces 50% of substance P from hNK1 receptors transfected in CHO or COS cells. In radioligand binding assays, Aprepitant is 3000-fold selective for the human cloned NK1 receptor versus the human cloned NK3 receptor and >50,000-fold selective over the human cloned NK2 receptor. In a range of assays at other human cloned G–protein coupled receptors, Aprepitant retains >50,000-fold selectivity for the human cloned NK1 receptor. Aprepitant is inactive in human monoamine oxidase A and B assays and at human serotonin 5–HT1A, 5–HT2A, 5–HT2c, 5–HT3, 5–HT5, 5–HT6, and 5–HT7 receptors (IC50>3 μM). In the PANLABS panel of radioligand binding screens using native animal tissues, Aprepitant inhibits [3H]substance P binding to native NK1 receptors in rat submaxillary gland; there are no significant interactions of Aprepitant with any other native animal G–protein coupled receptors or ion channels examined in the PANLABS screen. Aprepitant is inactive in monoamine uptake site (NE, 5–HT, DA) counterscreens using human and animal tissues (IC50> 3 μM)
In vivo
Aprepitant crosses the blood–brain barrier and occupied NK-1 receptors in the brain. Aprepitant has been shown to inhibit both acute and delayed emesis induced by cytotoxic chemotherapeutic such as cisplatin by blocking substance P. Aprepitant (3 mg/kg i.v. or p.o.) inhibits the emetic response to cisplatin (10 mg/kg i.v.). The anti-emetic protection afforded by Aprepitant (0.1 mg/kg i.v.) is enhanced by combined treatment with either dexamethasone (20 mg/kg i.v.) or the 5–HT3 receptor antagonist ondansetron (0.1 mg/kg i.v.). In a model of acute and delayed emesis, ferrets are dosed with cisplatin (5 mg/kg i.p.) and the retching and vomiting response recorded for 72 h. Pretreatment with Aprepitant (4–16 mg/kg p.o.) dose-dependently inhibits the emetic response to cisplatin. Once daily treatment with Aprepitant (2 and 4 mg/kg p.o.) completely prevents retching and vomiting in all ferrets tested. Further when daily dosing began at 24 h after cisplatin injection, when the acute phase of emesis had already become established, Aprepitant (4 mg/kg p.o. at 24 and 48 h after cisplatin) prevents retching and vomiting in three out of four ferrets. Aprepitant also plays a key part in transmission of pain impulses from the peripheral receptors to the CNS and is involved in various behavioural, neurochemical and cardiovascular responses to stress.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
L-754030
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Aprepitant (MK-0869)
生化机理
阿瑞匹坦（MK-0869，L-754030）是一种强效的选择性神经激肽-1 受体拮抗剂，IC50 为 0.1 nM。阿瑞匹坦可降低促炎细胞因子的水平，包括 G-CSF、IL-6、IL-8 和 TNFα。阿瑞匹坦可抑制艾滋病毒对人类巨噬细胞的感染。
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
神经激肽 1 受体拮抗剂
名称和识别符
EC号
677-636-6
分子类型
小分子
Isomeric SMILES
C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@@H]2[C@@H](N(CCO2)CC3=NNC(=O)N3)C4=CC=C(C=C4)F
分子量
534.43
Reaxy-Rn
14529316
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14529316&ln=
高级数据
产品属性
| ALogP | 4.2 |
|---|
关联靶点（人）
CYP3A4
Tclin
细胞色素P450 3A4(Cytochrome P450 3A4)
(1 活性数据)
TACR1
Tclin
P物质受体(Substance-P receptor)
(14 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 32 mg/mL warmed with 50ºC Water: bath (99.76 mM); DMSO: 21 mg/mL (65.47 mM); Ethanol: 4 mg/mL (12.47 mM);
比旋光度
69° (C=1,MeOH)
熔点
252 °C
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
Merck Index
753
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214607 |
分析证书 | A407946 |
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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