5-(N-乙基-N-异丙基)阿米洛利(EIPA), α 2A 肾上腺素受体的异构调节剂;ASIC1 的通道阻断剂;TRPP2 的通道阻断剂

CAS: 1154-25-2 货号: N132356 分子式: C11H18ClN7O 分子量: 299.76 EC号: 634-217-2
有货
级别和纯度: Moligand™ ? Moligand™ —— 阿拉丁的配体和生物活性小分子系列。适用于需要明确小分子工具的受体、通路和结合研究。 ≥95%
别名
5-(N-乙基-N-异丙基)阿米洛利
储存条件
-20°C储存
运输条件
超低温运输
★
规格
库存
价格
数量
5mg
N132356-5mg
现货 Stock Image
¥329.90
25mg
N132356-25mg
现货 Stock Image
¥899.90
100mg
N132356-100mg
期货 Stock Image
¥1,899.90
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为什么选择此级别

Moligand™ 级 提供 ≥95% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。

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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。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 39 篇同行评审文献引用。

概述

EIPA (L593754) 是一种具有口服活性的 TRPP3 通道抑制剂,IC50 为 10.5 μM。EIPA 可通过抑制 Na+/H+-exchanger 3 (NHE3) 来促进自噬 (autophagy)。EIPA 也抑制巨胞饮作用 (macropinocytosis)。EIPA 可用于炎症和癌症的研究,如胃癌、结肠癌、胰腺癌。


规格

别名
5-(N-乙基-N-异丙基)阿米洛利
英文别名
5-(Ethylisopropyl)amiloride | Ethylisopropyl amiloride | EU-0100045 | HY-101840 | SMR000326875 | Tox21_500045 | 3-Amino-N-(aminoiminomethyl)-6-chloro-5-(ethyl(1-methylethyl)amino)pyrazinecarboxamide | DTXSID80151084 | N-Amidino-3-amino-5-ethylisopropylami
规格或纯度
Moligand™, ≥95%
英文名称
EIPA
生化机理
TRPP3通道抑制剂(IC50 =10.5μM)。抑制Na + / H +交换剂(NHE)。阿米洛利的衍生物。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
通道阻滞剂
作用机制
α 2A 肾上腺素受体的异构调节剂;ASIC1 的通道阻断剂;TRPP2 的通道阻断剂
纯度
≥95%
名称和识别符
PubChem SID
EC号
634-217-2
分子类型
小分子
IUPAC Name
3-amino-6-chloro-N-(diaminomethylidene)-5-[ethyl(propan-2-yl)amino]pyrazine-2-carboxamide
INCHI
1S/C11H18ClN7O/c1-4-19(5(2)3)9-7(12)16-6(8(13)17-9)10(20)18-11(14)15/h5H,4H2,1-3H3,(H2,13,17)(H4,14,15,18,20)
InChi Key
QDERNBXNXJCIQK-UHFFFAOYSA-N
Smiles
CCN(C1=NC(=C(N=C1Cl)C(=O)N=C(N)N)N)C(C)C
Isomeric SMILES
CCN(C1=NC(=C(N=C1Cl)C(=O)N=C(N)N)N)C(C)C
分子量
299.76
Reaxy-Rn
8708046
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8708046&ln=

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

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批次质量数据。输入批号以获取对应 COA。

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高级数据

系统学分类

分类树(Taxonomy Tree)

界(kingdom) 有机化合物
超类(Superclass) 有机杂环化合物
类(Class) 二嗪类
亚类(Subclass) 吡嗪类
中间层级节点(Intermediate Tree Nodes) 吡嗪羧酸及其衍生物
直接上位类(Direct Parent) 吡嗪酰胺类
其他上位类(Alternative Parents) 二烷基芳胺  酰基胍  氨基吡嗪类  芳基氯化物  咪唑内酰胺类  乙烯基酰胺  杂芳族化合物  氨基酸及其衍生物  炔丙基型1,3-偶极有机化合物  氮杂环化合物  甲脒类  碳氢化合物衍生物  有机氧化物  有机氯化物  有机氧化合物  有机光子化合物  伯胺  
分子骨架(Molecular Framework) 芳香族杂单环化合物
取代基(Substituents) 酰基胍 - 氨基酸 - 氨基酸或其衍生物 - 氨基吡嗪 - 芳香族杂单环化合物 - 芳基氯化物 - 芳基卤化物 - 氮杂环 - 羧酰亚胺 - 羧酸衍生物 - 二烷基芳基胺 - 胍 - 杂芳香族化合物 - 烃衍生物 - 咪唑内酰胺 - 有机1,3-双极性化合物 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机氯化物 - 有机卤化物 - 有机氮化合物 - 有机氧化合物 - 有机氮化合物 - 初级胺 - 丙炔型1,3-双极性有机化合物 - 吡嗪甲酰胺 - 乙烯酰胺
描述(Description) 该化合物属于吡嗪羧酰胺类有机化合物。这类化合物含有吡嗪环,其上连接有羧酰胺基团。
外部描述符(External Descriptors) 暂无
三维结构
交互式化学结构模型





关联靶点(人)
SLC9A1 Tchem 钠/氢交换器 1(Sodium/hydrogen exchanger 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SLC9A5 Tchem 钠/氢交换器 5(Sodium/hydrogen exchanger 5) (6 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PKD2L1 Tchem 多囊肾病 2 类蛋白 1(Polycystic kidney disease 2-like 1 protein) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ADRA2A Tclin α-2A 肾上腺素受体(Alpha-2A adrenergic receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ASIC1 Tchem 酸敏感离子通道 1(Acid-sensing ion channel 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TSHR Tclin Thyroid stimulating hormone receptor (29986 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR5A Tchem Serotonin 5a (5-HT5a) receptor (1433 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ARSA Tbio Cerebroside-sulfatase (655 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALOX15B Tchem Arachidonate 15-lipoxygenase, type II (7244 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SMPD1 Tchem Sphingomyelin phosphodiesterase (13561 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GLP1R Tclin Glucagon-like peptide 1 receptor (111429 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC9A3 Tclin Sodium/hydrogen exchanger 3 (483 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC9A5 Tchem Sodium/hydrogen exchanger 5 (22 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEK293 (82097 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FEN1 Tchem Flap endonuclease 1 (12055 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
POLI Tchem DNA polymerase iota (116820 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 (345557 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
THPO Tbio Thrombopoietin (834 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GMNN Tbio Geminin (128009 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PMP22 Tbio Peripheral myelin protein 22 (699 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MBNL1 Tbio Muscleblind-like protein 1 (34431 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX1 Tbio Chromobox protein homolog 1 (92434 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MPHOSPH8 Tbio M-phase phosphoprotein 8 (656 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ATXN2 Tbio Ataxin-2 (54410 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
USP1 Tchem Ubiquitin carboxyl-terminal hydrolase 1 (22556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RGS4 Tchem Regulator of G-protein signaling 4 (13867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MEN1 Tchem Menin/Histone-lysine N-methyltransferase MLL (48157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Opioid receptors; mu & delta (1530 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PAX8 Tchem Paired box protein Pax-8 (1910 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
关联靶点(其它种属)
SLC9A1 Sodium/hydrogen exchanger 1 (3 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC9A2 Sodium/hydrogen exchanger 2 (9 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Saccharomyces cerevisiae (19171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NHE1 Sodium/hydrogen exchanger (7 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Txnrd1 Thioredoxin reductase 1, cytoplasmic (45279 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FTL Ferritin light chain (43324 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
作用机制
作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献
化学和物理性质
溶解性
溶于DMSO, 最高浓度 (mg/mL): 29.98, 最高浓度(mM): 100;溶于1eq. HCl, 最高浓度 (mg/mL): 14.99, 最高浓度(mM): 50
分子量
299.760 g/mol
XLogP3
1.300
氢键供体数Hydrogen Bond Donor Count
3
氢键受体数Hydrogen Bond Acceptor Count
5
可旋转键计数Rotatable Bond Count
4
精确质量Exact Mass
299.126 Da
单同位素质量Monoisotopic Mass
299.126 Da
拓扑极表面积Topological Polar Surface Area
137.000 Ų
重原子数Heavy Atom Count
20
形式电荷Formal Charge
0
复杂度Complexity
372.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
0
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
安全和危险性(GHS)
象形图
信号词
警告
危险声明

H315: 引起皮肤刺激

H319: 引起严重眼睛刺激

H335: 可能引起呼吸道刺激

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P264: 处理后要彻底洗手。

P271: 仅在室外或通风良好的地方使用。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P321: 特殊处理(请参阅此标签上的...)。

P302+P352: 如皮肤沾染:用水充分清洗。

P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。

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。

P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。

P405: 密闭存放

P403+P233: 存放在通风良好的地方。保持容器密闭。

P501: 将内容物/容器处理到。。。

P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。

P337+P317: 如果眼睛刺激持续:寻求医疗帮助。

P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。

P319: 如果你感到不适,请寻求医疗帮助。

WGK Germany
3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
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批号(Lot Number) 证书类型 货号
B2309422 分析证书 N132356
B2309424 分析证书 N132356
B2603434 分析证书 N132356
B2603435 分析证书 N132356
B2603437 分析证书 N132356
A2426043 分析证书 N132356
J2531353 分析证书 N132356
J2531381 分析证书 N132356
J2531502 分析证书 N132356
G2525090 分析证书 N132356
D2526015 分析证书 N132356
B2309418 分析证书 N132356
E2408044 分析证书 N132356
F2307397 分析证书 N132356
J2310204 分析证书 N132356
J2429189 分析证书 N132356

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技术文档和文章
此产品的引用文献
引用文献
1. Xucan Yang, Lulu Cheng, Yile Zhao, Haoran Ma, Haitao Song, Xuanmin Yang, Kang-Nan Wang, Yanrong Zhang.  (2023)  Aggregation-induced emission-active iridium (III)-based mitochondria-targeting nanoparticle for two-photon imaging-guided photodynamic therapy.  JOURNAL OF COLLOID AND INTERFACE SCIENCE,  [PMID:38176241] [10.1016/j.jcis.2023.12.172]
2. Dan Yuan, Qi Li, Qibo Zhang, Feibai Zhou, Qiangzhong Zhao, Mouming Zhao.  (2023)  Enhanced curcumin transportation across epithelial barrier by mucus-permeable soy protein nanoparticles-mediated dual transcytosis pathways.  FOOD CHEMISTRY,  [PMID:37897825] [10.1016/j.foodchem.2023.137771]
3. Xin Chang, Chang Liu, Yu-Mo Han, Qiu-Ling Li, Bin Guo, Hu-Lin Jiang.  (2023)  Efficient transfected liposomes co-loaded with pNrf2 and pirfenidone improves safe delivery for enhanced pulmonary fibrosis reversion.  Molecular Therapy-Nucleic Acids,  [PMID:37159604] [10.1016/j.omtn.2023.04.006]
4. Wu Wenting, Ding Quan, Zhou Zhiwei, Kuang Wenliang, Jiang Lipeng, Liu Peng, Ai Weiping, Zhu Weifeng.  (2023)  Transcellular Transport Behavior of the Intact Polymeric Mixed Micelles with Different Polymeric Ratios.  AAPS PHARMSCITECH,  24  (2): (1-16).  [PMID:36792796] [10.1208/s12249-022-02454-y]
5. Hou Zhenyu, Zhou Mei, Ma Yuanyuan, Xu Xiaoxuan, Zhang Zhiqi, Lai Shiwei, Fan Wenpei, Xie Jinbing, Ju Shenghong.  (2022)  Size-changeable nanoprobes for the combined radiotherapy and photodynamic therapy of tumor.  EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,  49  (8): (2655-2667).  [PMID:35536421] [10.1007/s00259-022-05830-9]
6. Xiudan Wang, Junya Lu, Yuling Mao, Qinfu Zhao, Caishun Chen, Jianan Han, Meiqi Han, Huijuan Yuan, Siling Wang.  (2022)  A mutually beneficial macrophages-mediated delivery system realizing photo/immune therapy.  JOURNAL OF CONTROLLED RELEASE,  [PMID:35489548] [10.1016/j.jconrel.2022.04.038]
7. Mingming Song, Shuqi Dong, Xiaofei An, Wenxiang Zhang, Ning Shen, Yanbo Li, Caixia Guo, Chang Liu, Xiao Li, Siyu Chen.  (2022)  Erythrocyte-biomimetic nanosystems to improve antitumor effects of paclitaxel on epithelial cancers.  JOURNAL OF CONTROLLED RELEASE,  [PMID:35381274] [10.1016/j.jconrel.2022.03.060]
8. Min Li, Sanpeng Li, Yixuan Huang, Haixia Chen, Songya Zhang, Zhicheng Zhang, Weigang Wu, Xiaobin Zeng, Boping Zhou, Bin Li.  (2021)  Secreted Expression of mRNA-Encoded Truncated ACE2 Variants for SARS-CoV-2 via Lipid-Like Nanoassemblies.  ADVANCED MATERIALS,  33  (34): (2101707).  [PMID:34278613] [10.1002/adma.202101707]
9. Yu Zhang, Junxi Liu, Pengfei Dou, Zhijing Wu, Ziming Zheng, Xianglin Pan, Tao Zhou, Kaiping Wang.  (2021)  Oral absorption characteristics and mechanisms of a pectin-type polysaccharide from Smilax china L. across the intestinal epithelium.  CARBOHYDRATE POLYMERS,  [PMID:34364625] [10.1016/j.carbpol.2021.118383]
10. Zhuqing Dai, Jiangfeng Song, Ye Chen, Lei Feng, Yayuan Xu, Dajing Li, Caie Wu, Zhongyuan Zhang, Jun Liu.  (2021)  Study on the bioavailability of stevioside-encapsulized lutein and its mechanism.  FOOD CHEMISTRY,  [PMID:33756320] [10.1016/j.foodchem.2021.129528]
11. Guo Shiqi, Liang Yanzi, Liu Lanze, Yin Miaomiao, Wang Aiping, Sun Kaoxiang, Li Youxin, Shi Yanan.  (2021)  Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics.  JOURNAL OF NANOBIOTECHNOLOGY,  19  (1): (1-21).  [PMID:33499885] [10.1186/s12951-021-00770-2]
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本产品的 CAS 号为 1154-25-2,分子式为 C11H18ClN7O,分子量为 299.76 g/mol。InChIKey QDERNBXNXJCIQK-UHFFFAOYSA-N。
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