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GS967, Na 抑制剂 v1.5

钠通道抑制剂
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
G421101-1ml
1ml 现货 Stock Image

基本描述

英文别名 GS4589671,​2,​4-​Triazolo[4,​3-​a]​pyridine,6-​[4-​(trifluoromethoxy)​phenyl]​-​3-​(trifluoromethyl)​-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 GS967
生化机理 GS967 (GS458967)是一种强效的晚期INa选择性抑制剂,具有抗心律失常作用。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 Na 抑制剂 v1.5
产品介绍


Information

GS967 GS967 (GS458967) is a potent and selective inhibitor of late I Na with anti-arrhythmic actions.

Targets

late INa 0.13 μM

In vitro

GS967 (3 μM) has no significant effect on L- or T-type calcium channel currents or Na+-Ca2+ exchanger current (INCX), and 1 μM GS967 has minimal or no effect on the ATP-inhibited K+ current or on human cardiac ion channels expressed in human embryonic kidney 293 or Chinese hamster ovary cells. GS967 is a novel sodium channel modulatorspecifically developed to inhibit persistent sodium current, with a 42-fold preference for persistent as opposed to peakcurrent inhibition.

In vivo

GS967 protects against seizures and prematurelethality in vivo. Chronic GS967 does not cause overt behavioraltoxicity or sedation in wild-type mice at theeffective anticonvulsant dose. GS967 suppresses arrhythmogenicity evoked by ischemia, hypokalemia, and catecholamines in canine and porcine models.

产品属性

ALogP 5.307
hba_count 3
Rotatable Bond 4

关联靶点(人)

SCN2A Tclin 钠通道蛋白 2 型亚基 α(Sodium channel protein type 2 subunit alpha) (2 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)
SCN5A Tclin 钠通道蛋白 5 型亚基 α(Sodium channel protein type 5 subunit alpha) (4 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)
SCN1A Tclin 钠通道蛋白 1 型亚基 α(Sodium channel protein type 1 subunit alpha) (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)
SCN1A Tclin Sodium channel protein type I alpha subunit (483 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
SCN5A Tclin Sodium channel protein type V alpha subunit (3462 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
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)

Scn2a Sodium channel protein type II alpha subunit (191 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn3a Sodium channel protein type III alpha subunit (24 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn9a Sodium channel protein type IX alpha subunit (69 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn8a Sodium channel protein type VIII alpha subunit (53 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn10a Sodium channel protein type X alpha subunit (425 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Scn4a Sodium channel protein type IV alpha subunit (55 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Oryctolagus cuniculus (11301 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
Cynomolgus monkey (4946 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
Liver microsome (341 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 6-[4-(trifluoromethoxy)phenyl]-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
INCHI 1S/C14H7F6N3O/c15-13(16,17)12-22-21-11-6-3-9(7-23(11)12)8-1-4-10(5-2-8)24-14(18,19)20/h1-7H
InChi Key FEVBKJITJDHASC-UHFFFAOYSA-N
Smiles C1=CC(=CC=C1C2=CN3C(=NN=C3C(F)(F)F)C=C2)OC(F)(F)F
Isomeric SMILES C1=CC(=CC=C1C2=CN3C(=NN=C3C(F)(F)F)C=C2)OC(F)(F)F
MeSH Entry Terms 6-(4-(trifluoromethoxy)phenyl)-3-(trifluoromethyl)(1,2,4)triazolo(4,3-a)pyridine;GS-458967;GS-967;GS967
分子量 347.22
Reaxy-Rn 21012437
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21012437&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 45
DMSO(mM) Max Solubility 129.600829445308
Water(mg / mL) Max Solubility <1
分子量 347.210 g/mol
XLogP3 4.900
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 9
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 347.049 Da
单同位素质量Monoisotopic Mass 347.049 Da
拓扑极表面积Topological Polar Surface Area 39.400 Ų
重原子数Heavy Atom Count 24
形式电荷Formal Charge 0
复杂度Complexity 435.000
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 GHS07
信号词 警告
危险声明

H302: 吞食有害

H315: 引起皮肤刺激

H320: 引起眼睛刺激

H335: 可能引起呼吸道刺激

预防措施声明

P264: 处理后要彻底洗手。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P330: 漱口

P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。

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