17
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T20993 |
Memantine
|
Others | Others |
Memantine 是口服具有活性的、非竞争性的N-甲基-D-天冬氨酸受体拮抗剂,可用于研究中重度阿尔茨海默病。 | |||
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。 | |||
T27949 |
LY382884
LY-382884,LY 382884 |
GluR | Neuroscience |
LY382884 是一种具有选择性和有效性的 GLU(K5)受体拮抗剂,具有抗焦虑活性。LY382884可阻断阻断苔藓纤维LTP的诱导。 | |||
TP1924L1 |
ZIP acetate(863987-12-6 free base)
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
ZIP acetate(863987-12-6 free base) 是一种新型的细胞渗透性蛋白激酶 Mζ (PKMζ) 抑制剂,它是一种参与 LTP 维持的组成型活性非典型 PKC 同工酶。在体外选择性阻断 PKMζ 诱导的海马切片突触增强。逆转晚期 LTP (IC50 = 1 - 2.5 μM) 并在体内中央给药后导致 1 天前的空间记忆持续丧失。 | |||
TP1895L1 |
KYL acetate(676657-00-4 free base)
|
Ephrin Receptor | Tyrosine Kinase/Adaptors |
KYL acetate(676657-00-4 free base) 是EphA4受体酪氨酸激酶抑制剂(Kd = 0.8 μM);抑制 EphA4-EphrinA5 相互作用 (IC50 = 6.34 μM)。防止 AβO 诱导的突触损伤、树突棘丢失并防止海马 CA3-CA1 传输中 LTP 的阻断。在细胞培养基中表现出较长的半衰期(在 PC3 和 C2C12 培养基中分别为 8 和 12 小时)。它有神经保护作用。 | |||
T21995 |
XAP044
|
GluR | Neuroscience |
XAP044 是高效的选择性mGlu7拮抗剂。代谢型谷氨酸受体亚型 7 是哺乳动物 CNS 中神经传递的重要突触前调节剂。它在啮齿动物行为测试中表现出较好的大脑暴露、广谱抗应激、抗抑郁以及抗焦虑作用。 | |||
T41142 |
EM 163
|
IL Receptor; p38 MAPK; MyD88 | Immunology/Inflammation; MAPK |
EM 163是一种 TIR-TIR 相互作用抑制剂,它是MyD88蛋白的TIR(Toll/白细胞介素-1受体)结构域拟态。EM 163针对IL-1受体中的TIR 结构域,阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B(SEB)引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中,EM 163阻断p38的激活和IL-1β对化学诱导的长期电位(LTP)引发的蛋白质合成的抑制作用。 | |||
T24779 | SEN-1269 | ||
SEN-1269 is an amyloid-β (AB) aggregation inhibitor that acts by blocking Aβ(1-42) aggregation and protecting neuronal cell lines exposed to Aβ(1-42), reducing Aβ oligomer-induced LTP and memory deficits in vivo. | |||
TP1924 |
ZIP
|
||
Novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-phase LTP (IC50 = 1 | |||
TP1990 |
Norleual
|
||
Angiotensin IV analog. Highly potent HGF/c-MET inhibitor (IC50 = 3 pM). Inhibits HGF-induced MDCK cell proliferation and invasion in vitro. Also AT4 receptor antagonist; disrupts LTP stabilization. Antiangiogenic. | |||
TP2007 |
Lei-Dab7
Lei-Dab 7 |
||
High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive | |||
T28653 |
S-8510 free base
SB 737552,SB-737552,S8510,SB737552,S-8510,S 8510 |
||
S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced | |||
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。 | |||
TP1895 |
KYL peptide
KYL |
||
KYL peptide is an EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM); inhibits EphA4-EphrinA5 interactions (IC50 = 6.34 μM). Prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective. | |||
T75946 |
Lei-Dab7 TFA
|
||
Lei-Dab7 TFA, a selective and high-affinity blocker of the K Ca 2.2 (SK2) channel with a dissociation constant (K d) of 3.8 nM, demonstrates over 200-fold selectivity for K Ca 2.2 compared to K Ca 2.1, K Ca 2.3, K Ca 3.1, K v, and Kir2.1. Furthermore, Lei-Dab7 TFA enhances theta-burst responses and long-term potentiation (LTP) in rat hippocampal slices in vitro. | |||
T71651 |
GSK1370319A
|
||
GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-relate... | |||
T79718 |
CaMKIIα-PHOTAC
|
CaMK | Neuroscience |
CaMKIIα-PHOTAC是一种靶向Ca2+/钙调蛋白依赖性蛋白激酶IIα(CaMKIIα)的光化学靶向嵌合体(PHOTAC)。该分子在特定波长光照射下实现靶蛋白的泛素化及通过蛋白酶体催化的降解。CaMKIIα-PHOTAC能在光照条件下显著降低小鼠海马区域的诱发LTP反应强度,减弱突触功能,并对维护亚细胞级别的树突结构域、长时程增强及记忆能力起到关键作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1601 |
Effusol
灯心草菲酚,厄弗酚 |
Caspase | Apoptosis; Proteases/Proteasome |
Effusol 是一种从 Juncus effuses 中分离到的酚类物质,对 DPPH 自由基(IC50:79 μM) 及 ABTS 自由基(IC50:2.73 μM)具有较强的清除活性。它能挽救皮质酮减弱的 CA1 LTP,保护海马功能对抗应激诱导的认知能力下降。 |