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26

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9723 GluR6 antagonist-1

Src Angiogenesis; Tyrosine Kinase/Adaptors
GluR6 antagonist-1 抑制酪氨酸激酶 p56lck SH2 结构域的 pY 结合位点。
T82295 GluR23Y

GluR23Y是一种具有生物活性的肽,应用于ELISA细胞表面测定,专用于监测培养的海马神经元内AMPA受体在胰岛素刺激下的内吞情况。该肽能够阻止由胰岛素引起的AMPA受体数量的下降。通过将GluR23Y与HIV-1的膜转导结构域融合,实现对神经元的传递,从而有效抑制了胰岛素诱导的效应。
T80246 TAT-GluR23A Fusion Peptide

TAT-GluR23A Fusion Peptide 是一种肽,具有特定的生物活性。该化合物由 GluR23A 序列结合至 TAT 蛋白转导结构域(PTD),其中 GluR23A 为 GluR23Y(一种无生物活性肽,用于抑制谷氨酸受体的内吞)的突变体,其由氨基酸 869 至 877 构成,并将 Tyr 用 Ala 代替,移除了关键的磷酸化位点。
T15090 Decoglurant

RO4995819

GluR Neuroscience
Decoglurant (RO4995819) 是 mGluR2和 mGluR3的负变构调制器,有抗抑郁作用。
T12717 Basimglurant

CTEP Derivative,RG7090

GluR Neuroscience
Basimglurant (CTEP Derivative) 是一种高效,选择性,可口服的 mGlu5负变构调节剂,Kd 值为1.1 nM。
T35028 Valiglurax

VU2957,VU 0652957,VU 2957,VU-0652957,VU0652957,VU-2957

GluR Neuroscience
Valiglurax (VU2957),也称为 VU0652957和 VU2957,是一种强效、选择性、中枢神经系统渗透剂,可口服生物利用的 mGlu4正变构调节剂。VU2957具有良好的跨物种的体内外药理学和药代动力学性质。VU2957被评估为治疗帕金森病的临床前开发候选药物。
T9970 mGluR3 modulator-1

1-ethyl-3-(morpholin-4-yl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile,1-乙基-3-(1,4-氧杂氮杂环己-4-基)-5,6,7,8-四氢异喹啉-4-甲腈

GluR Neuroscience
mGluR3 modulator-1 (1-ethyl-3-(morpholin-4-yl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile) 是 mGluR3 的正变构调节剂,可用于治疗帕金森病的研究。
T38612 Linaprazan glurate

Others Others
Linaprazan glurate 抑制外源性或内源性刺激的胃酸分泌。 Linaprazan glurate 可用于胃肠道炎症性疾病和消化性溃疡疾病的研究。
T11951 Mavoglurant racemate

AFQ-056 racemate

Others Others
Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist. Mavoglurant (racemate) is the racemate of mavoglurant.
T11311 Foliglurax monohydrochloride

PXT002331 (monohydrochloride)

Others Others
Foliglurax monohydrochloride Antiparkinsonian effect. is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM.
T11311L Foliglurax

PXT002331

GluR Neuroscience
Foliglurax is a highly selective brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) (EC50: 79 nM).
T61277 mGluR2 modulator 4

mGluR2 modulator 4 (compound 47) is a highly potent positive allosteric modulator of mGluR2, exhibiting an EC 50 value of 0.8 μM. It holds the potential for investigating antipsychotic properties [1].
T81801 mGluR5 antagonist-1

mGluR5 antagonist-1,一种高亲和力的mGluR5拮抗剂,其IC50为11.5 nM,表现出抗抑郁活性。
T32080 Histidine oxoglurate

Histidine alpha-ketoglutarate

Histidine oxoglurate is a bioactive chemical.
T17241 Auglurant

VU0424238

Others Others
Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration.
T38910 mGluR2 antagonist 1

mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies.
T60882 mGluR2 modulator 2

mGluR2 modulator 2 (compound 2) 可用于抗精神病药物研究。mGluR2 modulator 2 是一种有效的、选择性和口服生物可利用的mGluR2正变构调节剂,EC50值为 0.13 μM。
T15134 Dipraglurant

ADX48621

Others Others
Dipraglurant 是一种可透过血脑屏障的 mGluR5 的负变构调节剂 (NAM),具有有效性,选择性和口服活性,其 IC50 值为 21 nM。Dipraglurant 可治疗帕金森病左旋多巴诱导的运动障碍(PD-LID)。
T62202 mGluR2 modulator 1

mGluR2 modulator 1 (compound 95) 是一种有效的、具有血脑屏障通透性的 mGluR2 (代谢型谷氨酸受体-2)正向变构调节剂 (EC50: 0.03 μM)。mGluR2 modulator 1 能够用于研究精神病。
T34282 Remeglurant

Remeglurant is used as a selective antagonist of the mGlu5 receptor.
T38659 mGluR5 modulator 1

mGluR5 modulator 1 is a compound that acts as a positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). Its primary application lies in the field of schizophrenia and cognitive impairment research.
T6562 Latrepirdine dihydrochloride

Dimebolin dihydrochloride,Latrepirdine,Latrepirdine 2HCl,Dimebolin

Beta Amyloid; 5-HT Receptor; Adrenergic Receptor; GluR; Autophagy; Histamine Receptor Autophagy; GPCR/G Protein; Immunology/Inflammation; Neuroscience
Latrepirdine dihydrochloride (Dimebolin dihydrochloride) 是一种具有口服活性和神经活性的多种药物靶点的拮抗剂,可刺激淀粉样前体蛋白分解代谢和 β-淀粉样蛋白分泌。
T3486 3-MATIDA

GluR; NMDAR Neuroscience
3-MATIDA 是一种有效的 mGluR-1 拮抗剂(IC50:6.3 μM,大鼠 mGluR-1a)。显示出 ≥ 40 倍于其他受体的选择性:mGluR-5、mGluR-2、mGluR-4 (mGluR-4a) (IC50 > 300 μM)、NMDA 和 GluR (AMPA) (IC50 = 250 μM)。 3-MATIDA 在体外培养的鼠皮质细胞和大鼠海马切片培养物中充当神经保护剂。
T14130 Adomeglivant

LY2409021

Glucagon Receptor GPCR/G Protein
Adomeglivant (LY2409021) 是一种高效的选择性胰高血糖素受体 (GluR) 变构拮抗剂,主要用于2型糖尿病的研究。
T81912 LSP-GR3

iGluR Membrane transporter/Ion channel; Neuroscience
LSP-GR3为一种新型化学修饰RNA寡核苷酸,亦即剪接调控寡聚体(SMOs),可特异性调控中枢神经系统内GluR的选择性剪接及GluR3-flip表达。
T76278 Efinopegdutide

Efinopegdutide (JNJ-64565111) 是一种高效的胰高血糖素样肽-1 (GLP-1) /胰高血糖素受体 (GluR) 双重激动剂,具有同时激活GLP-1和胰高血糖素受体的能力,主要用于非酒精性脂肪性肝炎 (NASH) 的研究领域。

化合物

GluR6 antagonist-1
Cat.No: T9723
Synonym:
Target: Src
GluR23Y
Cat.No: T82295
Synonym:
Target:
TAT-GluR23A Fusion Peptide
Cat.No: T80246
Synonym:
Target:
Decoglurant
Cat.No: T15090
Synonym: RO4995819
Target: GluR
Basimglurant
Cat.No: T12717
Synonym: CTEP Derivative,RG7090
Target: GluR
Valiglurax
Cat.No: T35028
Synonym: VU2957,VU 0652957,VU 2957,VU-0652957,VU0652957,VU-2957
Target: GluR
mGluR3 modulator-1
Cat.No: T9970
Synonym: 1-ethyl-3-(morpholin-4-yl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile,1-乙基-3-(1,4-氧杂氮杂环己-4-基)-5,6,7,8-四氢异喹啉-4-甲腈
Target: GluR
Linaprazan glurate
Cat.No: T38612
Synonym:
Target: Others
Mavoglurant racemate
Cat.No: T11951
Synonym: AFQ-056 racemate
Target: Others
Foliglurax monohydrochloride
Cat.No: T11311
Synonym: PXT002331 (monohydrochloride)
Target: Others
Foliglurax
Cat.No: T11311L
Synonym: PXT002331
Target: GluR
mGluR2 modulator 4
Cat.No: T61277
Synonym:
Target:
mGluR5 antagonist-1
Cat.No: T81801
Synonym:
Target:
Histidine oxoglurate
Cat.No: T32080
Synonym: Histidine alpha-ketoglutarate
Target:
Auglurant
Cat.No: T17241
Synonym: VU0424238
Target: Others
mGluR2 antagonist 1
Cat.No: T38910
Synonym:
Target:
mGluR2 modulator 2
Cat.No: T60882
Synonym:
Target:
Dipraglurant
Cat.No: T15134
Synonym: ADX48621
Target: Others
mGluR2 modulator 1
Cat.No: T62202
Synonym:
Target:
Remeglurant
Cat.No: T34282
Synonym:
Target:
mGluR5 modulator 1
Cat.No: T38659
Synonym:
Target:
Latrepirdine dihydrochloride
Cat.No: T6562
Synonym: Dimebolin dihydrochloride,Latrepirdine,Latrepirdine 2HCl,Dimebolin
Target: Beta Amyloid, 5-HT Receptor, Adrenergic Receptor, GluR, Autophagy, Histamine Receptor
3-MATIDA
Cat.No: T3486
Synonym:
Target: GluR, NMDAR
Adomeglivant
Cat.No: T14130
Synonym: LY2409021
Target: Glucagon Receptor
LSP-GR3
Cat.No: T81912
Synonym:
Target: iGluR
Efinopegdutide
Cat.No: T76278
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T8626 Transtorine

1,4-DIHYDRO-4-OXOQUINOLINE-2-CARBOXYLIC ACID,1,4-二氢-4-氧代喹啉-2-羧酸

GluR; NMDAR Neuroscience
Transtorine (1,4-DIHYDRO-4-OXOQUINOLINE-2-CARBOXYLIC ACID) 是一种 GluR 和 NMDA 抑制剂。
T20191 (-)-Camphoric acid

(-)-樟脑酸,L-Camphoric acid,Camphoric acid, (-)-

GluR Neuroscience
(-)-Camphoric acid (L-Camphoric acid) 是一种活性较低的樟脑酸对映异构体,樟脑酸可诱导 GluR 表达。

天然产物

Transtorine
Cat.No: T8626
Synonym: 1,4-DIHYDRO-4-OXOQUINOLINE-2-CARBOXYLIC ACID,1,4-二氢-4-氧代喹啉-2-羧酸
Target: GluR, NMDAR
(-)-Camphoric acid
Cat.No: T20191
Synonym: (-)-樟脑酸,L-Camphoric acid,Camphoric acid, (-)-
Target: GluR
TargetMol Loading
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