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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
T22517 5,7-Dichlorokynurenic acid

5,7-二氯犬尿喹啉酸,5,7-dichlorokynurenic acid sodium,5,7-DCKA

NMDAR Neuroscience
5,7-Dichlorokynurenic acid (5,7-dichlorokynurenic acid sodium) 是一种专门针对于NMDA 受体甘氨酸位点的竞争性拮抗剂(KB:65 nM)。它是犬尿酸的衍生物,可降低大鼠皮质细胞培养物中 NMDA 诱导的神经元损伤程度。
T1909 L-701324

7-氯-4-羟基-3-(3-苯氧基)苯基-2(1H)-喹啉,L701324

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
L-701324 是一种 NMDA 受体,对甘氨酸位点具有高亲和力和选择性,用作口服活性和长效抗惊厥药。
T16797 RPR104632

NMDAR Neuroscience
RPR104632 是一种新型有效的位于 NMDA 甘氨酸位点的拮抗剂,具有神经保护活性。
T26686 AV-101

L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine

NMDAR Neuroscience
AV-101 (4-Cl-KYN) 是 NMDA 受体甘氨酸位点的前药拮抗剂,具有抗抑郁活性,可减少 MPTP 猴子中左旋多巴诱导的运动障碍。
T11516 GV-196771A

NMDAR Neuroscience
GV-196771A 一种新型的NMDA受体甘氨酸位点拮抗剂,具有强大的抗痛觉过敏活性。
T22542 1-Aminocyclobutanecarboxylic acid

ACBC,1-氨基环丁烷羧酸

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
1-Aminocyclobutanecarboxylic acid (ACBC) 是一种NMDA 受体部分激动剂,作用于 NR1 甘氨酸位点。
T5819 Rapastinel Trifluoroacetate

Thr-Pro-Pro-Thr-NH2 Trifluoroacetate,GLYX-13 Trifluoroacetate

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) 是一种 NMDA 受体调节剂,具有甘氨酸位点部分激动剂性质,有研究抑郁症的潜力。
T10781 CGP 78608 hydrochloride

PAMQX

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
CGP 78608 hydrochloride 是 NMDA 受体甘氨酸结合位点的特异性拮抗剂 (IC50 = 6 nM)。 CGP 78608 hydrochloride 具有抗惊厥活性。 CGP 78608 hydrochloride 增强 GluN1/GluN3A 介导的甘氨酸电流(估计 EC50 = 26.3 nM)。
T3407L Rapastinel acetate

Rapastinel acetate (117928-94-6 Free base)

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
Rapastinel acetate 是 N-甲基-D-天冬氨酸 (NMDA) 受体的调节剂和甘氨酸位点的部分激动剂,具有长效抗抑郁作用。
T22900 L-701252

L-701,252

NMDAR Neuroscience
L-701252 是一种有效的甘氨酸位点 NMDA 受体拮抗剂,IC50 值为 420 nM。L-701252 对全脑缺血提供小范围的神经保护。
T60612 Neboglamine hydrochloride

Neboglamine (CR-2249, XY-2401) hydrochloride 是NMDA 受体甘氨酸位点的正向调节剂,具有口服活性,可用于研究精神分裂症。
T22798 Gavestinel

GV 150526,Gavestinel sodium salt

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
Gavestinel (GV 150526) 是一种非竞争性的 NMDA 受体拮抗剂,具有有效性、选择性和口服活性。Gavestinel 可与 NMDA 受体的甘氨酸位点结合,其结合亲和力(pKi 值)为 8.5。Gavestinel 可用于急性缺血性脑卒中研究。
T69263 HA-966 HCl

HA-966 HCl is an NMDA receptor complex glycine site antagonist.
T27504 GV-196771

GV-196771 selectively antagonize the glycine-binding site of the NMDA ionophore.
T10191 7-Chlorokynurenic acid sodium salt

7-CKA sodium salt

Others Others
7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the NMDA receptor (IC50: 0.56 μM). It is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles (Ki: 0.59 μ
T71018 MDL 100748

MDL 100748 is a glycine site antagonist of NMDA receptor.
T23603 ACEA1011

ACEA-1011,ACEA 1011

ACEA1011 is a glycine site NMDA receptor antagonist. It may have analgesic effects.
T68750 HA-966 trihydrate

HA-966 trihydrate is an NMDA receptor complex glycine site antagonist.
T69211 GW-468816

GW-468816 is a glycine site NMDA receptor antagonist.
T69949 CGP-78608

CGP-78608 is a glycine site-specific N-methyl-D-aspartate receptor antagonist prevents activation of the NMDA/NO/CGMP pathway by ammonia.
T79273 NMDA receptor antagonist 6

iGluR Membrane transporter/Ion channel; Neuroscience
NMDA receptor antagonist6 (compound 13b) 为针对甘氨酸结合位点的NMDA 受体拮抗剂,其展现出对PC12 细胞的神经保护功能,能够抵御NMDA引起的细胞损伤及细胞凋亡。
T15684 L-689560

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
L-689560 是 N-甲基-D-天冬氨酸受体(NMDA)的有效拮抗剂,抑制 NMDA 甘氨酸结合位点。它用于研究 NMDA 受体在正常神经系统过程以及疾病中的作用,也广泛用作结合研究中的放射性标记配体,也。
T35787 Obestatin (human) (trifluoroacetate salt)

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manne...
T35582 H-Arg-Gly-Asp-Cys-OH (trifluoroacetate salt)

H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection ...
T76378 RGD-4C

RGD-4C(ACDCRGDCFC)是一种携带Arg-Gly-Asp(RGD)序列的肽,具备与αv整合素结合的能力,用于模拟细胞外基质蛋白的整合素识别特性。作为αv整合素的配体,它能够与生物活性分子进行偶联,进而在动物模型中展现出抗肿瘤活性。
T82379 FN-A208 fusion peptide

FN-A208 是源自鼠层粘连蛋白 a1 的 A208 与纤连蛋白 (GRGDS) 活性位点和甘氨酸间隔区融合形成的生物活性肽。该肽能形成淀粉样原纤维,并有助于促进肌动蛋白应力纤维的形成,进而介导成纤维细胞附着,显示出其在组织再生和工程生物粘合剂方面的应用潜力。FN-A208 与 IKVAV 受体和整合素发生相互作用,而在 EDTA 存在下,其活性则会被破坏。

化合物

5,7-Dichlorokynurenic acid
Cat.No: T22517
Synonym: 5,7-二氯犬尿喹啉酸,5,7-dichlorokynurenic acid sodium,5,7-DCKA
Target: NMDAR
L-701324
Cat.No: T1909
Synonym: 7-氯-4-羟基-3-(3-苯氧基)苯基-2(1H)-喹啉,L701324
Target: NMDAR, iGluR
RPR104632
Cat.No: T16797
Synonym:
Target: NMDAR
AV-101
Cat.No: T26686
Synonym: L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine
Target: NMDAR
GV-196771A
Cat.No: T11516
Synonym:
Target: NMDAR
1-Aminocyclobutanecarboxylic acid
Cat.No: T22542
Synonym: ACBC,1-氨基环丁烷羧酸
Target: NMDAR, iGluR
Rapastinel Trifluoroacetate
Cat.No: T5819
Synonym: Thr-Pro-Pro-Thr-NH2 Trifluoroacetate,GLYX-13 Trifluoroacetate
Target: NMDAR, iGluR
CGP 78608 hydrochloride
Cat.No: T10781
Synonym: PAMQX
Target: NMDAR, iGluR
Rapastinel acetate
Cat.No: T3407L
Synonym: Rapastinel acetate (117928-94-6 Free base)
Target: NMDAR, iGluR
L-701252
Cat.No: T22900
Synonym: L-701,252
Target: NMDAR
Neboglamine hydrochloride
Cat.No: T60612
Synonym:
Target:
Gavestinel
Cat.No: T22798
Synonym: GV 150526,Gavestinel sodium salt
Target: NMDAR, iGluR
HA-966 HCl
Cat.No: T69263
Synonym:
Target:
GV-196771
Cat.No: T27504
Synonym:
Target:
7-Chlorokynurenic acid sodium salt
Cat.No: T10191
Synonym: 7-CKA sodium salt
Target: Others
MDL 100748
Cat.No: T71018
Synonym:
Target:
ACEA1011
Cat.No: T23603
Synonym: ACEA-1011,ACEA 1011
Target:
HA-966 trihydrate
Cat.No: T68750
Synonym:
Target:
GW-468816
Cat.No: T69211
Synonym:
Target:
CGP-78608
Cat.No: T69949
Synonym:
Target:
NMDA receptor antagonist 6
Cat.No: T79273
Synonym:
Target: iGluR
L-689560
Cat.No: T15684
Synonym:
Target: NMDAR, iGluR
Obestatin (human) (trifluoroacetate salt)
Cat.No: T35787
Synonym:
Target:
H-Arg-Gly-Asp-Cys-OH (trifluoroacetate salt)
Cat.No: T35582
Synonym:
Target:
RGD-4C
Cat.No: T76378
Synonym:
Target:
FN-A208 fusion peptide
Cat.No: T82379
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T10191L 7-Chlorokynurenic acid

7-chloro-4-hydroxy-2-carboxyquinoline,7-氯犬尿酸,7-CKA

GluR; NMDAR Neuroscience
7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) 是一种有效的选择性 NMDA 受体拮抗剂,对甘氨酸 B 激动剂位点的 IC50 为 0.56 μM。 7-Chlorokynurenic acid 抑制谷氨酸再摄取到突触小泡中,Ki 为 0.59 μM,并在神经轴输送后显示出镇痛作用。
T4752 1-Aminocyclopropane-1-carboxylic acid

1-Aminocyclopropanecarboxylic acid,1-氨基环丙烷羧酸,1-Amino-1-carboxycyclopropane,ACC

Endogenous Metabolite; NMDAR Metabolism; Neuroscience
1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。

天然产物

7-Chlorokynurenic acid
Cat.No: T10191L
Synonym: 7-chloro-4-hydroxy-2-carboxyquinoline,7-氯犬尿酸,7-CKA
Target: GluR, NMDAR
1-Aminocyclopropane-1-carboxylic acid
Cat.No: T4752
Synonym: 1-Aminocyclopropanecarboxylic acid,1-氨基环丙烷羧酸,1-Amino-1-carboxycyclopropane,ACC
Target: Endogenous Metabolite, NMDAR
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