Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7870 |
TCN 201
TCN-201 |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
TCN 201 是选择性的、有效的,非竞争性的GluN1/GluN2A NMDA 受体拮抗剂,pIC50值为 6.8。与 GluN1/GluN2B NMDA 受体 (pIC50<4.3) 相比,它对 GluN1/GluN2A NMDA 受体具有选择性。 | |||
T16801 |
(RS)-(Tetrazol-5-yl)glycine
LY 285265,D,L-(tetrazol-5-yl)glycine |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
(RS)-(Tetrazol-5-yl)glycine (LY 285265) 是一种高效且选择性的 N-甲基-D-天冬氨酸 (NMDA) 受体激动剂。它能够诱导小鼠癫痫发作反应和 Fos。它对 GluN1/GluN2D 和 GluN1/GluN2A 的EC50分别为 99 nM,1.7 μM。 | |||
T8450 |
TCN 213
TCN213 |
NMDAR | Neuroscience |
TCN 213 是一种可克服的(surmountable)、甘氨酸依赖的 GluN1/GluN2A NMDAR 选择性拮抗剂,当甘氨酸的含量为75、 750、7500 nM 时,IC50s 值分别为 0.55、3.5、40 μM。它可用于在药理学上监测 NMDAR 表达在发育中的皮层神经元中的转换。 | |||
T22748 |
DQP 1105
|
NMDAR | Neuroscience |
DQP 1105 是一种高效非竞争性NMDA 受体拮抗剂。DQP-1105 抑制含有 GluN2C (IC50:7.0 Μm) 和 GluN2D (IC50:2.7 Μm) 的受体 。 IC50值至少比重组 GluN2B-、GluN2A-、GluA1- 或 GluK2 受体低 50 倍。 | |||
T15407 |
GNE-0723
|
Others | Others |
GNE 0723 is an NMDAR brain permeable positive allosteric modulator (EC50: 21 nM for GluN2A; 7.4 and 6.2 μM for GluN2C and GluN2D, respectively). | |||
T15408 | GNE 5729 | Others | Others |
GNE 5729 is an NMDAR of brain permeable positive allosteric modulator (EC50: 37 nM for GluN2A; 4.7 and 9.5 μM for GluN2C and GluN2D, respectively). | |||
T31980 |
GNE-6901
GNE6901,GNE 6901 |
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GNE-6901 is a selective GluN2A PAM. | |||
T19881 |
UBP608
UBP-608,UBP 608 |
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UBP608 is an allosteric modulator of NMDA receptor family. It selectively inhibits GluN1/GluN2A receptors with a 23-fold selectivity compared to GluN1/GluN2D receptors. | |||
T28093 |
MPX-007
MPX 007 |
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MPX-007, a potent NMDA inhibitor, inhibits GluN2A-containing NMDA receptors expressed in HEK cells with IC50s of 27 nM. | |||
T31979 |
GNE-3476
GNE 3476 |
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GNE-3476 is an NMDA receptor PAM. Ge-3476 has different degrees of activity on different receptors.GNE-3476 has relatively low efficacy on GluN2A, some activity as an AMPAR PAM, and weak activity at GluN2B-containing receptors. | |||
T69906 |
PEAQX sodium
|
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PEAQX, also known as NVP-AAM077; is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors, more detailed studies of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests. | |||
T73491 | TP-050 | ||
TP-050 是一种口服有效的选择性 NMDAR 激动剂,抑制 GluN2A 和 GluN2D 的 EC50值分别为 0.51 μM 和 9.6 µM。TP-050 可穿过血脑屏障 (BBB)。TP-050 诱导海马区的长期增益效应 (LTP),增强神经元信号传输。 | |||
TP2060 |
Conantokin G
|
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GluN2B (formally NR2B) selective, competitive antagonist of the NMDA receptor. Blocks NMDA-evoked current in mouse cortical neurons (IC50 = 480 nM); also inhibits NMDA-evoked responses in oocytes expressing GluN2B (formally NR2B), but not GluN2A (formally | |||
T73359 |
NYX-2925
|
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NYX-2925 是一种口服有效的NMDAR 调节剂。NYX-2925 恢复 mPFC 中 GluN2A 和 GluN2B 上活化的Src 和Src 磷酸化位点的水平。NYX-2925 对 CAMKII 没有影响,也没有任何成瘾或镇静/共济失调的副作用。NYX-2925 可用于多种 NMDA 受体介导的中枢神经系统疾病的研究。 | |||
T61227 |
NAB-14
|
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NAB-14 is a powerful and selective chemical compound that acts as a non-competitive antagonist for GluN2C and GluN2D receptors. With an IC50 value of 580 nM for GluN1/GluN2D, NAB-14 demonstrates high potency. This compound exhibits a remarkable selectivity of more than 800-fold towards recombinant GluN2C and GluN2D when compared to GluN2A and GluN2B. Furthermore, NAB-14 possesses the ability to penetrate the blood-brain-barrier effectively [1]. |