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犬尿喹啉酸, GPR35 激动剂

内源性离子/烟碱拮抗剂
9篇引用文献 COA COA
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货号 (SKU) 包装规格 是否现货 价格 数量
K120012-250mg
 250mg 现货 Stock Image
K120012-1g
 1g 现货 Stock Image
K120012-5g
 5g 现货 Stock Image
K120012-25g
 25g 现货 Stock Image
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查看相关系列
Apoptosis (7108) Class A GPCR (8201) CXCR (82) Endogenous Metabolite (978) GPCR/G Protein (3179) GPR35 (14) GPR35 Agonist (8) Immunology/Inflammation (1938) Metabolic Enzyme/Protease (4889) 代谢物 (8911) 神经元信号传导 (3320) 离子型谷氨酸受体 (238) 离子通道 (4087) 膜转运器/离子通道 (1829)
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基本描述

别名 4-羟基-2-喹啉甲酸 | 4-羟基喹啉-2-甲酸 | 犬尿喹啉酸水合物 | 4-羟基喹啉-2-羧酸水合物
英文别名 AMY18102 | BDBM81975 | Oprea1_032085 | Tox21_500716 | HCZHHEIFKROPDY-UHFFFAOYSA- | LP00716 | KYA | 4-Hydroxy-2-quinolincarboxylic acid | 4-Hydroxyquinoline-2-carboxylic acid | BPBio1_001350 | CCRIS 4428 | HMS500P11 | KBio2_001596 | NINDS_000309 | Transtor
规格或纯度 Moligand™, ≥97%
英文名称 Kynurenic acid
生化机理 犬尿氨酸（KynA）是 N-甲基-d-天冬氨酸（NMDA）、α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）和凯因酸受体的非选择性拮抗剂。它能阻断凯尼克酸的神经毒性。犬尿氨酸还能阻断烟碱乙酰胆碱受体。它是色氨酸分解途径的副产品。犬尿氨酸是一种神经调节剂，可控制谷氨酸、多巴胺、乙酰胆碱和α-氨基丁酸（GABA）的水平。KynA 控制神经内分泌功能，KynA 水平的改变是抑郁症、精神分裂症、阿尔茨海默氏症和亨廷顿氏症的潜在标志。大脑中正常水平的 KynA 对认知功能至关重要。它是离子型、甘氨酸 β 和 α7 尼古丁受体的内源性拮抗剂。在体内具有神经保护作用。
应用 An antagonist of NMDA and AMPA/kainate receptors
储存温度 2-8°C储存
运输条件 冰袋运输
作用类型 激动剂
作用机制 GPR35 激动剂
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍
产品介绍：

Kynurenic acid is a metabolite of tryptophan in mammals via the kynurenine pathway. Studies have observed that Kynurenic acid acts as a ligand to the GPR35 G protein-coupled receptor. The binding of Kynurenic acid to GPR35 has been noted to affect calcium mobilization and inositol phosphatase synthesis and may indicate potential signaling functions by Kynurenic acid via the GPR35 receptor. Additionally reported to be a broad spectrum, excitatory amino acid (EAA) antagonist. Other studies have reported that Kynurenic acid acts as an antagonist to mammalian ionotropic glutamate receptors especially NMDA (N-methyl-D-aspartate receptors).Kynurenic acid is an inhibitor of AChR α7, GluR and GlyR.


产品用途：
An antagonist of NMDA and AMPA/kainate receptors
Kynurenic acid has been used as a constituent in dissection saline solution for embryonic cerebral cortical cells[7] and human primary astrocytes. It has also been used as a medium supplement for murine intestinal epithelial cell line, MODE-K and induced pluripotent stem cell (iPSC)-derived neurons cells.

Product Introduction

Kynurenic acid is a metabolite of tryptophan in mammals via the kynurenine pathway. Studies have observed that Kynurenic acid acts as a ligand to the GPR35 G protein-coupled receptor. The binding of Kynurenic acid to GPR35 has been noted to affect calcium mobilization and inositol phosphatase synthesis and may indicate potential signaling functions by Kynurenic acid via the GPR35 receptor. Additionally reported to be a broad spectrum, excitatory amino acid (EAA) antagonist. Other studies have reported that Kynurenic acid acts as an antagonist to mammalian ionotropic glutamate receptors especially NMDA (N-methyl-D-aspartate receptors).Kynurenic acid is an inhibitor of AChR α7, GluR and GlyR.


Product Usage

An antagonist of NMDA and AMPA/kainate receptors
Kynurenic acid has been used as a constituent in dissection saline solution for embryonic cerebral cortical cells[7] and human primary astrocytes. It has also been used as a medium supplement for murine intestinal epithelial cell line, MODE-K and induced pluripotent stem cell (iPSC)-derived neurons cells.
纯度 ≥97%

关联靶点（人）

GPR35 Tchem G蛋白偶联受体35(G-protein coupled receptor 35) (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)
CHRNA7 Tchem 神经元乙酰胆碱受体亚基 α-7(Neuronal acetylcholine receptor subunit alpha-7) (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)
AHR Tclin 芳烃受体(Aryl hydrocarbon 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)
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
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
CHRNA7 Tchem Neuronal acetylcholine receptor protein alpha-7 subunit (3524 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GLA Tclin Alpha-galactosidase A (5444 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AHR Tclin Aryl hydrocarbon receptor (1071 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NGFR Tclin Low affinity neurotrophin receptor p75NTR (32 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GAA Tclin Lysosomal alpha-glucosidase (35701 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALDH1A1 Tchem Aldehyde dehydrogenase 1A1 (77053 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
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
HSD17B10 Tchem Endoplasmic reticulum-associated amyloid beta-peptide-binding protein (20669 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
POLK Tbio DNA polymerase kappa (8653 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KDM4A Tchem Lysine-specific demethylase 4A (52245 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
APEX1 Tchem DNA-(apurinic or apyrimidinic site) lyase (38016 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
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
KDM4E Tchem Lysine-specific demethylase 4D-like (40243 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HPGD Tchem 15-hydroxyprostaglandin dehydrogenase [NAD+] (24926 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GPR35 Tchem G-protein coupled receptor 35 (2643 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
KMT2A Tchem Histone-lysine N-methyltransferase MLL (17327 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2672 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
BAZ2B Tchem Bromodomain adjacent to zinc finger domain protein 2B (56204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (2517 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
GRIN1 Tclin Glutamate [NMDA] receptor (933 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA-A receptor; agonist GABA site (140 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）

Slc17a1 Renal sodium-dependent phosphate transport protein 1 (33 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 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
Slc17a8 Vesicular glutamate transporter 3 (89 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pseudomonas aeruginosa (123386 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Enterobacter cloacae (7976 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Shigella flexneri (1836 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Proteus mirabilis (3894 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Bacillus subtilis (32866 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 norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
lef Anthrax lethal factor (7585 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
pfk 6-phospho-1-fructokinase (7870 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hippocampus (57 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 (6467 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Gria2 Glutamate receptor ionotropic, AMPA (2103 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Grik1 Glutamate receptor ionotropic, kainate (722 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Grin1 Glutamate receptors; NMDA/AMPA (104 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Gpr35 G protein-coupled receptor GPR35 (72 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

PubChem SID 504750720
EC号 207-751-5
分子类型 小分子
IIUPAC Name 4-oxo-1H-quinoline-2-carboxylic acid
INCHI 1S/C10H7NO3/c12-9-5-8(10(13)14)11-7-4-2-1-3-6(7)9/h1-5H,(H,11,12)(H,13,14)
InChi Key HCZHHEIFKROPDY-UHFFFAOYSA-N
Smiles C1=CC=C2C(=C1)C(=O)C=C(N2)C(=O)O
Isomeric SMILES C1=CC=C2C(=C1)C(=O)C=C(N2)C(=O)O
关联CAS 492-27-3
分子量 189.17
Beilstein号 147451
Reaxy-Rn 474479
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=474479&ln=

化学和物理性质

溶解性 Soluble in water (partly), hot alcohol, DMSO (75 mM), 0.1 M NaOH (50 mg/ml), and methanol.
熔点 275°C
分子量 189.170 g/mol
XLogP3 1.300
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 4
可旋转键计数Rotatable Bond Count 1
精确质量Exact Mass 189.043 Da
单同位素质量Monoisotopic Mass 189.043 Da
拓扑极表面积Topological Polar Surface Area 66.400 Ų
重原子数Heavy Atom Count 14
形式电荷Formal Charge 0
复杂度Complexity 308.000
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 Warning
WGK Germany 3
RTECS VB2080000
Merck Index 5327
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
F2527118 分析证书 K120012
I2207837 分析证书 K120012
I2207839 分析证书 K120012
I2207840 分析证书 K120012
I2207841 分析证书 K120012
D2501052 分析证书 K120012
K2208219 分析证书 K120012
K2208222 分析证书 K120012
K2208223 分析证书 K120012
K2208224 分析证书 K120012
H2413049 分析证书 K120012

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引用文献

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