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PF-03463275

    级别和纯度:
  • ≥99%
有货

库存信息

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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
P649439-5mg
5mg 期货 Stock Image
P649439-10mg
10mg 期货 Stock Image
P649439-50mg
50mg 期货 Stock Image

基本描述

英文别名 1-Methyl-1H-imidazole-4-carboxylic acid(3-chloro-4-fluoro-benzyl)-(3-methyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amide | N-[(3-chloro-4-fluorophenyl)methyl]-1-methyl-N-[[(1R,5S)-3-methyl-3-azabicyclo[3.1.0]hexan-6-yl]methyl]imidazole-4-carboxamide | 117323
规格或纯度 ≥99%
英文名称 PF-03463275
生化机理 PF-03463275 是一种中枢渗透性、口服型、选择性和竞争性 GlyT1(甘氨酸转运体-1)可逆抑制剂,其 K i 为 11.6 nM。PF-03463275 具有研究精神分裂症的潜力。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a K i of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.

In Vivo

PF-03463275 (1-10 mg/kg; s.c.) attenuates oscillatory potentials (OPs). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley ratsDosage: 1, 3 and 10 mg/kg Administration: S.c. Result: A dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from the dark-adapted rats.

Form:Solid

纯度 ≥99%

关联靶点(人)

SLC6A9 Tchem 钠和氯依赖性甘氨酸转运蛋白 1(Sodium- and chloride-dependent glycine transporter 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)
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
SLC6A5 Tchem Glycine transporter 2 (697 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)

Slc6a9 Glycine transporter 1 (255 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
MDCK (10148 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 N-[(3-chloro-4-fluorophenyl)methyl]-1-methyl-N-[[(1R,5S)-3-methyl-3-azabicyclo[3.1.0]hexan-6-yl]methyl]imidazole-4-carboxamide
INCHI 1S/C19H22ClFN4O/c1-23-7-13-14(8-23)15(13)9-25(19(26)18-10-24(2)11-22-18)6-12-3-4-17(21)16(20)5-12/h3-5,10-11,13-15H,6-9H2,1-2H3/t13-,14+,15?
InChi Key KYLOBHXXQOZRKK-YIONKMFJSA-N
Smiles CN1CC2C(C1)C2CN(CC3=CC(=C(C=C3)F)Cl)C(=O)C4=CN(C=N4)C
Isomeric SMILES CN1C[C@@H]2[C@H](C1)C2CN(CC3=CC(=C(C=C3)F)Cl)C(=O)C4=CN(C=N4)C
关联CAS 1173239-39-8
PubChem CID 44156901
MeSH Entry Terms 1-methyl-1H-imidazole-4-carboxylic acid (3-chloro-4-fluoro-benzyl)-(3-methyl-3-aza-bicyclo(3.1.0) hex-6-ylmethyl)amide;PF-03463275;PF-3463275
分子量 376.86

化学和物理性质

溶解性 DMSO : 33.33 mg/mL (88.44 mM; Need ultrasonic)
分子量 376.900 g/mol
XLogP3 2.400
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 4
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 376.147 Da
单同位素质量Monoisotopic Mass 376.147 Da
拓扑极表面积Topological Polar Surface Area 41.400 Ų
重原子数Heavy Atom Count 26
形式电荷Formal Charge 0
复杂度Complexity 526.000
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 2
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)

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