FP802（8 μM，24–72 小时）能有效破坏 NMDAR/TRPM4 复合物，并在细胞模型中发挥神经保护作用，但它并不直接促进或抑制神经突生长 [1]。FP802（10 μM，30 分钟）表现出显著的神经保护作用，能够抵抗谷氨酸（20 μM）介导的毒性（IC50 = 8.7 µM），并将 NMDA 抑制的早期基因表达恢复至生理水平 [2]。FP802 在 HEK293 细胞中未显示出对 NMDAR 的拮抗活性（GluN1/GluN2A 和 GluN1/GluN2B 的 IC50 均 > 250 mM）[2]。 FP802（30 分钟）能够剂量依赖性地阻断散发性 ALS 疾病特异性诱导多能干细胞 (iPSC) 衍生的前脑类器官中 NMDA 诱导的神经元有丝分裂后死亡 [2]。

FP802 (10 和 40 mg/kg，表皮，每日一次，持续 4 个月) 可改善 5xFAD 小鼠的认知功能、防止元结构损伤并减少淀粉样蛋白病理[1]。 FP802 (40 mg/kg，皮下注射，每日一次，约第 15 周起持续 4 周) 通过 NMDAR/TRPM4 复合物，能够安全地阻止 ALS运动神经元缩短并延长其生存期[2]。

实时定量PCR[1]
细胞类型： 小鼠皮层神经元
测试浓度： 10 μM
孵育时间： 30 分钟
实验结果： 消除了 eNMDARs 诱导的转录关闭，并增强了 NMDA 灌注诱导的即刻早期基因 (IEG) Atf3、Arc、Bdnf、cFos、抑制素β A 和 Npas4 的表达，使其达到与比库啉诱导的动作电位爆发相当的水平。

Animal/Disease Models: 5xFAD transgenic mice and wild-type littermates[1]
Doses: 10 and 40 mg/kg
Route of Administration: p.o., daily for 4 months
Experimental Results: Showed no apparent adverse effects on the liver, kidney, or heart. Reduced the complex formation of GluN2B with TRPM4 in the 5xFAD mice at both 10 and 40 mg/kg. Reduced complex formation of GluN2A with TRPM4 at 40 mg/kg. Significantly decreased the interaction between NMDAR and TRPM4 without affecting the total protein levels of GluN2A, GluN2B, or TRPM4. Led to a significant increase in the time 5xFAD mice spent in the target quadrant and the frequency with which they crossed the platform's prior location at the dose of 40 mg/kg, compared to vehicle. Increased the time 5xFAD mice spent exploring the novel object in the Novel Object Recognition (NOR) test and the displaced object in the Novel Location Recognition (NLR) test relative to vehicle treatment. Prevented the shift of mitochondrial morphologies from normal to pathological phenotypes in both CA1 and CA3. Effectively preserved dendritic trees in 5xFAD mice as compared to controls, as demonstrated by increased total dendritic length and numbers of crossings in the Sholl analysis. Prevented the increase in the density of 'apparent orphaned synapses' in both stratum oriens (CA1 basal dendrites) and stratum radiatum (CA1 apical dendrites) of 5xFAD mice. Prevented the loss of excitatory and inhibitory synapses and the associated structural deterioration of postsynaptic densities (PSD) in the basal and apical dendrites of CA1 neurons, thereby preserving synaptic integrity in 5xFAD mice. Led to a 25-40% reduction in Aβ plaque load, significantly limiting plaque development without completely preventing its formation.

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Animal/Disease Models: Male SOD1G93A transgenic mice and wild-type littermates[2]
Doses: 40 mg/kg
Route of Administration: s.c., daily from ~week 15 for 4 weeks
Experimental Results: Disrupted he interaction of TRPM4 with the NMDAR subunit GluN2B in mice spinal cord. Significantly better neurological scores and less body weight loss than vehicle-treated controls. Significantly improved motor performance (increased total distance traveled and rearing frequency in the open field). Significantly extended the lifespan of SOD1G93A mice (survival median increased from 151 to 164 days). Preserved larger soma sizes of lumbar spinal motor neurons compared to the control group at week 19. Significantly reduced serum NfL levels while showing no effect on spinal microglial response or EAAT2 expression. Showed no adverse effects on liver, kidney, heart, or blood counts.

[1]. https://pubmed.ncbi.nlm.nih.gov/40858778/

[2]. https://pubmed.ncbi.nlm.nih.gov/38325382/

C11H17CLN2

212.72

61694-81-3

FP802 dihydrochloride

Typically exists as solids at room temperature

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。