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依利罗地

非竞争性和GluN2B选择性NMDA拮抗剂
    级别和纯度:
  • ≥98%(HPLC)
有货

库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
E137445-10mg
10mg 现货 Stock Image
E137445-50mg
50mg 现货 Stock Image

基本描述

英文别名 ?-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol | BDBM50079387 | SL-82,0715; SL82,0715; SL 82,0715; SL-820715; SL820715; SL 820715 | Eliprodil, >=98% (HPLC), powder | HY-12881 | YW62A6TW29 | 1-Piperidineethanol, alpha-(4-chlorophenyl)-4-
规格或纯度 ≥98%(HPLC)
英文名称 Eliprodil
生化机理 在多胺调节位点起作用的非竞争性NMDA受体拮抗剂。对含GluN2A(NR2A)和GluN2C(NR2C)的受体具有选择性(对于IC50值分别为1,> 100和>100μM)。也是σ1配体(Ki =0.013μM)。拮抗神经元电压门控的Ca2 +通道,并选择性抑制延迟整流器K +电流(IKr)的快速分量。具有神经保护作用。有关最新命名约定,请参阅《 IUPHAR药理学指南》。
储存温度 2-8°C储存
运输条件 冰袋运输
产品介绍

Eliprodil is a non-competitive NMDA receptor antagonist which acts at the polyamine modulatory site. Eliprodil is selective for NMDA epsilon 2 (NR2B-containing receptors) over NR2A- and NR2C-containing receptors (IC50 values are 1, > 100 and > 100 μM respectively) in addition to acting as a Sigma Receptor (σ1 ligand) (Ki = 0.013 μM). Eliprodil antagonizes neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). Furthermore, Eliprodil is reported to act as a neuroprotective.

Eliprodil is a non-competitive NMDA receptor antagonist which acts at the polyamine modulatory site. Eliprodil is selective for NMDA epsilon 2 (NR2B-containing receptors) over NR2A- and NR2C-containing receptors (IC50 values are 1, > 100 and > 100 μM respectively) in addition to acting as a Sigma Receptor (σ1 ligand) (Ki = 0.013 μM). Eliprodil antagonizes neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). Furthermore, Eliprodil is reported to act as a neuroprotective.

纯度 ≥98%(HPLC)

关联靶点(人)

GRIN2B Tclin 谷氨酸受体离子型,NMDA 2B(Glutamate receptor ionotropic, NMDA 2B) (8 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
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 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
GRIN2B Tclin Glutamate [NMDA] receptor subunit epsilon 2 (467 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
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NFKB1 Tclin Nuclear factor NF-kappa-B p105 subunit (1459 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALOX15 Tchem Arachidonate 15-lipoxygenase (7108 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
GRIN2C Tclin Glutamate [NMDA] receptor subunit epsilon 3 (47 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TP53 Tchem Cellular tumor antigen p53 (48468 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U2OS (164939 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
HepG2 (196354 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BLM Tchem Bloom syndrome protein (4248 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
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
ATAD5 Tbio ATPase family AAA domain-containing protein 5 (122566 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate NMDA receptor; GRIN1/GRIN2B (726 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEK-293T (167025 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)

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
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus (17 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SIGMAR1 Sigma-1 receptor (3326 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npsr1 Neuropeptide S receptor (260 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
Impa1 Inositol monophosphatase 1 (16203 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
PGAM 2,3-bisphosphoglycerate-independent phosphoglycerate mutase (46 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Adra1b Adrenergic receptor alpha-1 (5652 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Grin1 Glutamate NMDA receptor; Grin1/Grin2a (798 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Grin1 Glutamate NMDA receptor; Grin1/Grin2c (1127 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tmem97 Sigma intracellular receptor 2 (922 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

名称和识别符

分子类型 小分子
IIUPAC Name 1-(4-chlorophenyl)-2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethanol
INCHI 1S/C20H23ClFNO/c21-18-5-3-17(4-6-18)20(24)14-23-11-9-16(10-12-23)13-15-1-7-19(22)8-2-15/h1-8,16,20,24H,9-14H2
InChi Key GGUSQTSTQSHJAH-UHFFFAOYSA-N
Smiles C1CN(CCC1CC2=CC=C(C=C2)F)CC(C3=CC=C(C=C3)Cl)O
Isomeric SMILES C1CN(CCC1CC2=CC=C(C=C2)F)CC(C3=CC=C(C=C3)Cl)O
分子量 347.85
Reaxy-Rn 7717696
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7717696&ln=

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 8.7, 最高浓度(mM): 25
分子量 347.900 g/mol
XLogP3 4.500
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 3
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 347.145 Da
单同位素质量Monoisotopic Mass 347.145 Da
拓扑极表面积Topological Polar Surface Area 23.500 Ų
重原子数Heavy Atom Count 24
形式电荷Formal Charge 0
复杂度Complexity 359.000
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 1
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 GHS07,   GHS09
信号词 警告
危险声明

H319: 引起严重眼睛刺激

H400: 对水生生物有剧毒

H410: 对水生生物有剧毒并具有长期持续影响

预防措施声明

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。

P391: 收集溢出物

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。

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。

WGK Germany 3
个人防护装备 Eyeshields, Gloves

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批号(Lot Number) 证书类型 货号
J1613010 分析证书 E137445
H1813139 分析证书 E137445

溶液计算器