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) |
|---|
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
Naftopidil 是选择性α1-肾上腺素能受体拮抗剂，或α受体抑制剂，Ki为58.3 nM。N α-1-Adrenergic receptor antagonist and an antihypertensive.
Information
Naftopidil (KT-611) is a selectiveα1-adrenergic receptorantagonist withKiof 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia.
In vitro
Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil induces p21(cip1) but not p27(kip1) in PC-3 cells. Naftopidil induces apoptosis in all the investigated malignant mesothelioma cells, and a similar effect is obtained with prazosin, another α1-adrenoceptor blocker. Naftopidil-induced reduction in cell viability is inhibited by GF109203X, while prazosin-induced in cell viability is less affected. Naftopidil, an alpha 1-adrenoreceptor antagonist produces a concentration-dependent inhibition ofcollagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 mM Naftopidil. Naftopidil also inhibits the adrenaline-induced rise in [Ca2+]i in a concentration-dependent manner (30 mM doxazosin), significant inhibitions of platelet aggregation also being produced. Naftopidil (0.3, 1, and 3 μM) inhibits 5-HT-induced bladder contraction in a concentration-dependent manner. Naftopidil inhibits both the 5-HT(2A) and 5-HT(2) receptor agonists-induced bladder contractions. Naftopidil binds to the human 5-HT(2A) and 5-HT(2B) receptors with pKi values of 6.55 and 7.82, respectively.
In vivo
Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats.
Cell Data
cell lines：Human monocytes
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
英文别名
KT-611 | 4-(2-methoxyphenyl)-α-[(1-naphthalenyloxy)methyl]-1-piperazineethanol
规格或纯度
10mM in DMSO
英文名称
Naftopidil
生化机理
萘夫地尔（KT-611）是一种选择性α1-肾上腺素能受体拮抗剂，对α1a、α1b和α1d的Ki分别为3.7 nM、20 nM和1.2 nM，用于治疗良性前列腺增生。
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
α-1d肾上腺素能受体拮抗剂
名称和识别符
EC号
692-531-5
分子类型
小分子
Isomeric SMILES
COC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O
分子量
392.5
Beilstein号
23(5)2,135
Reaxy-Rn
629965
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=629965&ln=
技术文档
高级数据
产品属性
| ALogP | 4.1 |
|---|
关联靶点（人）
ADRA1B
Tclin
α-1B 肾上腺素受体(Alpha-1B adrenergic receptor)
(1 活性数据)
ADRA1D
Tclin
α-1D 肾上腺素受体(Alpha-1D adrenergic receptor)
(3 活性数据)
ADRA1A
Tclin
α-1A 肾上腺素受体(Alpha-1A adrenergic receptor)
(4 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 33 mg/mL (198.53 mM); Water: 33 mg/mL warmed with 50ºC Water: bath (198.53 mM); Ethanol: 33 mg/mL (198.53 mM);
熔点
127°C
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H361: 怀疑破坏生育力或未出生的孩子
预防措施声明
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。。。
P203: 使用前，获取、阅读并遵守所有安全说明。
P318: 如果暴露或担心，请就医。
RTECS
TL9336500
Merck Index
6356
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
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