2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel iGluR
  4. FP802

FP802 是一种口服的强效 TwinF 界面抑制剂，可破坏并解除 NMDAR/TRPM4 死亡复合物的毒性。FP802 在 5xFAD 阿尔茨海默病 (AD) 小鼠模型中发挥强大的神经保护作用，可防止认知功能衰退、维持神经元结构完整性、减少 β- 淀粉样蛋白斑块形成并减轻线粒体病变。在肌萎缩侧索硬化 (ALS) 小鼠模型中，FP802 能阻止运动神经元丢失、降低血清神经丝轻链 (NfL) 水平、改善运动表现并小鼠延长寿命。FP802 可用于阿尔茨海默病和肌萎缩侧索硬化症的相关研究[1][2]。

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FP802

FP802 Chemical Structure

CAS No. : 61694-81-3

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FP802 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FP802 is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex. FP802 exerts powerful neuroprotective effects in the 5xFAD mouse model of Alzheimer’s disease (AD) by preventing cognitive decline, preserving neuronal structural integrity, reducing amyloid-β plaque formation, and mitigating mitochondrial pathology[1].FP802 stops loss of motor neurons, reduces serum neurofilament light chain (NfL) levels, improves motor performance, and extends life in a mouse model of amyotrophic lateral sclerosis (ALS)[2]. FP802 can be used for AD and ALS research[1][2].

体外研究
(In Vitro)

FP802 (8 μM, 24-72 h) 能有效破坏 NMDAR/TRPM4 复合物并在细胞模型中提供神经保护，但它本身并不直接促进或抑制神经突的生长[1]。
FP802 (10 μM，30 分钟) 表现出强大的神经保护作用，可抵抗谷氨酸 (20 μM) 介导的毒性 (IC50 = 8.7 µM)，并将 NMDA 抑制的即刻早期基因表达恢复到生理水平[2]。
FP802在 HEK293 细胞中对 NMDAR未显示拮抗活性 (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 NMDA 诱导的散发性 ALS 疾病特异性诱导多能干细胞 (iPSCs) 来源前脑类器官中神经元的有丝分裂后死亡[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FP802 相关抗体:

Real Time qPCR[1]

Cell Line: mouse cortical neurons
Concentration: 10 μM
Incubation Time: 30 min
Result: Eliminated the transcriptional shut-off induced by eNMDARs and boosted the NMDA bath application-induced expression of the immediate-early genes (IEGs) Atf3, Arc, Bdnf, cFos, Inhibin beta A, and Npas4 to reach levels that were comparable to those achieved by Bicuculline (HY-N0219)-induced action potential bursting.
体内研究
(In Vivo)

FP802 (10 和 40 mg/kg，口服，每日一次，持续 4 个月) 可改善 5xFAD 小鼠的认知功能、防止神经元结构退化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) 通过靶向 NMDAR/TRPM4 复合物，能够安全地阻止 ALS 小鼠运动神经元退化并延长其生存期[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SOD1G93A transgenic mice and wild-type littermates[2]
Dosage: 40 mg/kg
Administration: s.c., daily from ~week 15 for 4 weeks
Result: 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.
Animal Model: 5xFAD transgenic mice and wild-type littermates[1]
Dosage: 10 and 40 mg/kg
Administration: p.o., daily for 4 months
Result: 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.
分子量

212.72

Formula

C11H17ClN2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FP802 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FP80261694-81-3FP 802FP-802TRP ChanneliGluRTransient receptor potential channelsIonotropic glutamate receptorsTwinF interface inhibitorNMDAR/TRPM4neuroprotective5xFADADamyloid-β plaquemitochondrialNfLALSiPSCsorganoidsInhibitorinhibitorinhibit

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