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 3 篇同行评审文献引用。
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 | 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one
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=
技术文档
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）
信号词
Warning
危险声明
H319: 引起严重眼睛刺激
H351: 怀疑引起遗传缺陷
H373: 通过长时间或反复暴露对器官造成损害
H410: 对水生生物有剧毒并具有长期持续影响
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P273: 避免释放到环境中。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
P391: 收集溢出物
P203: 使用前，获取、阅读并遵守所有安全说明。
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P318: 如果暴露或担心，请就医。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
P319: 如果你感到不适，请寻求医疗帮助。
Merck Index
753
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:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 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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