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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
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.
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].
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。
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。
T15090 Decoglurant

RO4995819

GluR Neuroscience
Decoglurant (RO4995819) 是 mGluR2mGluR3的负变构调制器,有抗抑郁作用。
T10432L AZD-8529 mesylate

GluR Neuroscience
AZD-8529 mesylate 是高度选择性的可口服mGluR2正向调节剂,EC50值为 285 nM。它在 20-25 M 时,对 mGluR1、3、4、5、6、7 和 8 亚型没有显示正变构调节剂反应。
T3479 (RS)-MCPG

alpha-MCPG,(±)-MCPG

GluR Neuroscience
(RS)-MCPG ((±)-MCPG) 是一种竞争性和选择性 I/II 组代谢型谷氨酸受体 (mGluR) 拮抗剂,可阻断 TBS 诱导的幼年和新生大鼠海马神经元的转变。
T15812 LY2979165

mGlu2 agonist

GluR Neuroscience
LY2979165 (mGlu2 agonist) 是 mGluR2 的正构激动剂,可用于作为抗抑郁药的研究。
T3484 trans-ACPD

Trans-(±)-ACP,1-amino-1,3-dicarboxycyclopentane,(±)-trans-ACPD

GluR Neuroscience
trans-ACPD ((±)-trans-ACPD) 是代谢型受体激动剂,可促进钙离子活动及产生内向电流。
T27932 LY-2300559

LY2300559

GluR Neuroscience
LY-2300559 是代谢型谷氨酸受体 2 (mGluR2) 的激动剂,可用于偏头痛治疗的研究。
T6022 LY404039

pomaglumetad

Glucocorticoid Receptor; GluR Endocrinology/Hormones; Neuroscience
LY404039 (pomaglumetad) 是可口服的mGluR2mGluR3选择性激动剂,有抗精神病和抗焦虑的作用。它对重组人mGluR2mGluR3的Ki 分别为 149 和 92 nM,比对其他受体/转运蛋白的抑制性高 100 倍以上。
T41301 L-Cysteinesulfinic acid monohydrate

GluR Neuroscience
L-Cysteinesulfinic acid monohydrate 是代谢型谷氨酸受体 (mGluRs) 的有效激动剂,可以作用于 mGluR1,mGluR2mGluR5,mGluR4,mGluR6 和 mGluR8,pEC50分别为 3.92,3.9,4.6,2.7,4.0,和 3.94。
T3464 PHCCC

(-) PHCCC

GluR Neuroscience
PHCCC ((-) PHCCC) 是 I 组代谢型谷氨酸受体拮抗剂和 mGluR4 的正变构调节剂。 它对 mGluR2mGluR8 也有很强的拮抗作用,具有抗帕金森病作用。
T27448 GSK1331258

GSK 1331258,GSK-1331258

GSK1331258 is a selective, orally bioavailable positive modulators of mGluR2.
T10432 AZD-8529

Others Others
AZD-8529 is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
T23294 (S)-4C3HPG

Others Others
group I mGlu1a/1a receptor antagonist and mGluR2 agonist
T27449 GSK1331268

GSK 1331268,GSK-1331268

GSK1331268 is a selective, orally bioavailable positive modulators of mGluR2.
T27942 LY307452

LY 307452,LY-307452

LY307452 is a selective antagonist of mGluR2/3.
T14615 Biphenylindanone A

BINA

GluR Neuroscience
Biphenylindanone A is a selective potentiator of human mGluR2 (hmGluR2),and for the treatment of neurological disorders.
T28600 Ro4491533

Ro 4491533,Ro-4491533

Ro4491533 is a potent and selective negative allosteric modulator for group II of the metabotropic glutamate receptors (mGluR2/3).
T79302 MK-8768

MK-8768为口服生效且能穿越血脑屏障的选择性mGluR2负向变构调节剂,其IC50为9 nM。
T28034 MGS-0039

BCI 632,BCI-632,MGS0039,BCI632

MGS-0039 is a group II metabotropic glutamate receptor (mgluR2/3) antagonist. Antidepressant-like action of group II mGlu receptor antagonists does not depend on serotonergic system activation. However, the AMPA receptor seems to play a key role in the an
T60611 Talaglumetad hydrochloride

Talaglumetad (hydrochloride) 是Eglumegad 的前药,Eglumegad 是II 型代谢型谷氨酸受体(mGluR2/3)有效选择性的激动剂,用于治疗焦虑等精神疾病。
T62756 LY487379

LY487379是一种选择性的人类 mGluR2 阳性异生调节剂(PAM)。LY487379 可提高谷氨酸刺激的 [35 S] GTPγS 结合,作用于 mGlu2 受体 (EC50: 1.7 μM) 和 mGlu3 受体 (EC50>10 μM)。LY487379 在大鼠模型中促使认知的灵活性,并诱导行为抑制。LY487379 能够用于研究精神分裂症。
T9353 OXOMEMAZINE

AChR; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Oxomemazine 是毒菌碱 M1 受体的选择性拮抗剂,具有明显的抗毒蕈碱活性。它是基于吩噻嗪的组胺 H1 受体阻滞剂,是抗组胺和抗胆碱能试剂,可用于咳嗽相关研究。
T15816 LY341495

GluR Neuroscience
LY341495 是高效的代谢型谷氨酸受体拮抗剂,对多种谷氨酸受体的亚型表现除很高的活性,可用于研究神经系统疾病。
T23515 VU-29

VU 29

GluR Neuroscience
VU-29 是代谢型谷氨酸 5(mGlu5)受体的正变构调节剂,对 rmGluR5 的 EC50为 9 nM,Ki 为 244 nM。相对于其他亚型,它对 mGluR5 具有选择性,对 rmGluR1/rmGluR2和 hmGluR4的 EC50分别为557 nM/1.5 μM 和 154 nM。
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-2mGluR-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。
T15618 JNJ-46281222

GluR Neuroscience
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator). It has nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
T11165 EGLU

(2S)-α-EGLU,(2S)-α-Ethylglutamic acid

Others Others
EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent.EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist.
T15807 LY2794193

SGLT GPCR/G Protein
LY2794193 is a highly effective and selective agonist of the mGlu3 receptor (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).
T11906 LY 541850

GluR Neuroscience
LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells.
T15809 LY2812223

LIM Kinase Cell Cycle/Checkpoint
LY2812223 is a highly effective and functionally selective mGlu2 receptor agonist. It has a mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
T11911 LY3020371 hydrochloride

GluR Neuroscience
LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.
T38791 LY3020371

LY3020371 is a highly potent and selective antagonist targeting the glutamate (mGlu) 2/3 receptor, showcasing excellent inhibition at Ki values of 5.26 nM and 2.50 nM for hmGluR2 and hmGluR3, respectively. With its remarkable affinity and specificity, LY3020371 serves as a valuable tool in depression research.

化合物

mGluR2 antagonist 1
Cat.No: T38910
Synonym:
Target:
mGluR2 modulator 4
Cat.No: T61277
Synonym:
Target:
mGluR2 modulator 2
Cat.No: T60882
Synonym:
Target:
mGluR2 modulator 1
Cat.No: T62202
Synonym:
Target:
Decoglurant
Cat.No: T15090
Synonym: RO4995819
Target: GluR
AZD-8529 mesylate
Cat.No: T10432L
Synonym:
Target: GluR
(RS)-MCPG
Cat.No: T3479
Synonym: alpha-MCPG,(±)-MCPG
Target: GluR
LY2979165
Cat.No: T15812
Synonym: mGlu2 agonist
Target: GluR
trans-ACPD
Cat.No: T3484
Synonym: Trans-(±)-ACP,1-amino-1,3-dicarboxycyclopentane,(±)-trans-ACPD
Target: GluR
LY-2300559
Cat.No: T27932
Synonym: LY2300559
Target: GluR
LY404039
Cat.No: T6022
Synonym: pomaglumetad
Target: Glucocorticoid Receptor, GluR
L-Cysteinesulfinic acid monohydrate
Cat.No: T41301
Synonym:
Target: GluR
PHCCC
Cat.No: T3464
Synonym: (-) PHCCC
Target: GluR
GSK1331258
Cat.No: T27448
Synonym: GSK 1331258,GSK-1331258
Target:
AZD-8529
Cat.No: T10432
Synonym:
Target: Others
(S)-4C3HPG
Cat.No: T23294
Synonym:
Target: Others
GSK1331268
Cat.No: T27449
Synonym: GSK 1331268,GSK-1331268
Target:
LY307452
Cat.No: T27942
Synonym: LY 307452,LY-307452
Target:
Biphenylindanone A
Cat.No: T14615
Synonym: BINA
Target: GluR
Ro4491533
Cat.No: T28600
Synonym: Ro 4491533,Ro-4491533
Target:
MK-8768
Cat.No: T79302
Synonym:
Target:
MGS-0039
Cat.No: T28034
Synonym: BCI 632,BCI-632,MGS0039,BCI632
Target:
Talaglumetad hydrochloride
Cat.No: T60611
Synonym:
Target:
LY487379
Cat.No: T62756
Synonym:
Target:
OXOMEMAZINE
Cat.No: T9353
Synonym:
Target: AChR, Histamine Receptor
LY341495
Cat.No: T15816
Synonym:
Target: GluR
VU-29
Cat.No: T23515
Synonym: VU 29
Target: GluR
3-MATIDA
Cat.No: T3486
Synonym:
Target: GluR, NMDAR
JNJ-46281222
Cat.No: T15618
Synonym:
Target: GluR
EGLU
Cat.No: T11165
Synonym: (2S)-α-EGLU,(2S)-α-Ethylglutamic acid
Target: Others
LY2794193
Cat.No: T15807
Synonym:
Target: SGLT
LY 541850
Cat.No: T11906
Synonym:
Target: GluR
LY2812223
Cat.No: T15809
Synonym:
Target: LIM Kinase
LY3020371 hydrochloride
Cat.No: T11911
Synonym:
Target: GluR
LY3020371
Cat.No: T38791
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T11803 L-Cysteinesulfinic acid

Others Others
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs, pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively).

天然产物

L-Cysteinesulfinic acid
Cat.No: T11803
Synonym:
Target: Others
TargetMol Loading
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