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产品名称 | eNOS ↓ ↑ | iNOS ↓ ↑ | nNOS ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
1400W 2HCl |
+
eNOS, Ki: 50 μM |
++++
iNOS, Kd: <7 nM |
++
nNOS, Ki: 2 μM |
99%+ | |||||||||||||||
L-NAME HCl |
+++
eNOS, Ki: 39 nM |
++
iNOS, Ki: 4.4 μM |
+++
nNOS, Ki: 15 nM |
98% | |||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | AMPA receptor ↓ ↑ | GluR ↓ ↑ | mGluR5 ↓ ↑ | NMDA receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Evans Blue | ✔ | 85% (Dye content) | |||||||||||||||||
IEM-1754 |
+
GluR1, IC50: 6 μM GluR3, IC50: 6 μM |
99% | |||||||||||||||||
Latrepirdine 2HCl | ✔ | 99% | |||||||||||||||||
(-)-Huperzine A |
+++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
CTEP |
++++
mGlu5, IC50: 2.2 nM |
98%+ | |||||||||||||||||
MPEP |
++
mGluR5, IC50: 36 nM |
99%+ | |||||||||||||||||
Riluzole | ✔ | 97% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | IC87201, at concentrations ranging from 500 to 1800 μM, does not block the interactions between the PDZ domains (PDZ1, PDZ2, PDZ3) of PSD-95 and nNOS-PDZ, nor does it attach to the standard PDZ ligand-binding sites. Instead, IC87201 targets the β-finger of nNOS-PDZ, resulting in an allosteric inhibition of the nNOS-PDZ/PSD-95-PDZ interaction. Additionally, when TAMRA-nNOS is used as a probe, IC87201 generates a significant fluorescence-based artefactual signal[1]. IC87201, at a concentration of 20 μM, inhibits the formation of cGMP that is stimulated by NMDA compared to the control, in neurons cultured from the hippocampus[2]. IC87201, at concentrations of 10 and 100 nM, mitigates the reduction in neurite outgrowth induced by NMDA/glycine. It also decreases NMDA-stimulated cGMP production in primary hippocampal neurons (DIV 14-21) in a dose-dependent manner, with an IC50 value of (2.7 \mu M). Furthermore, IC87201 enhances branching in these neurons at concentrations of 10-30 μM compared to neurons treated with the control[3]. |
Animal study | Administered intraperitoneally at doses of 1, 4, and 10 mg/kg, IC87201 does not impair spatial working memory or source memory[2]. IC87201, at a dosage of 1 mg/kg, is efficacious in alleviating thermal hyperalgesia induced by NMDA in mice. This is associated with a peak plasma concentration of 55 ng/mL[3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.23mL 0.65mL 0.32mL |
16.17mL 3.23mL 1.62mL |
32.35mL 6.47mL 3.23mL |
CAS号 | 866927-10-8 |
分子式 | C13H10Cl2N4O |
分子量 | 309.151 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 105 mg/mL(339.64 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
动物实验配方 |