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

FP802 hydrochloride 是一种口服有效的强效 TwinF 界面抑制剂，可破坏并解除 NMDAR/TRPM4 死亡复合物的毒性。FP802 hydrochloride 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 hydrochloride 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 hydrochloride 可用于阿尔茨海默病和肌萎缩侧索硬化症的相关研究。

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FP802 dihydrochloride

FP802 dihydrochloride Chemical Structure

CAS No. : 2490401-57-3

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5 mg ￥476
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10 mg ￥765
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25 mg ￥1530
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50 mg ￥2448
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100 mg ￥3910
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FP802 dihydrochloride 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 dihydrochloride is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex. FP802 dihydrochloride 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 dihydrochloride 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 dihydrochloride can be used for AD and ALS research[1][2].

体外研究
(In Vitro)

FP802 (8 μM，24-72 小时) hydrochloride 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) hydrochloride 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 hydrochloride 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) hydrochloride 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 dihydrochloride 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) dihydrochloride 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) dihydrochloride 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: 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.
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.
分子量

285.64

Formula

C11H19Cl3N2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

H2O 中的溶解度 : 116.67 mg/mL (408.45 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5009 mL 17.5046 mL 35.0091 mL
5 mM 0.7002 mL 3.5009 mL 7.0018 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

FP802 dihydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.5009 mL 17.5046 mL 35.0091 mL 87.5228 mL
5 mM 0.7002 mL 3.5009 mL 7.0018 mL 17.5046 mL
10 mM 0.3501 mL 1.7505 mL 3.5009 mL 8.7523 mL
15 mM 0.2334 mL 1.1670 mL 2.3339 mL 5.8349 mL
20 mM 0.1750 mL 0.8752 mL 1.7505 mL 4.3761 mL
25 mM 0.1400 mL 0.7002 mL 1.4004 mL 3.5009 mL
30 mM 0.1167 mL 0.5835 mL 1.1670 mL 2.9174 mL
40 mM 0.0875 mL 0.4376 mL 0.8752 mL 2.1881 mL
50 mM 0.0700 mL 0.3501 mL 0.7002 mL 1.7505 mL
60 mM 0.0583 mL 0.2917 mL 0.5835 mL 1.4587 mL
80 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0940 mL
100 mM 0.0350 mL 0.1750 mL 0.3501 mL 0.8752 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • 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:

FP8022490401-57-3FP 802FP-802TRP ChanneliGluRTransient receptor potential channelsIonotropic glutamate receptorsTwinF interface inhibitorNMDAR/TRPM4neuroprotective5xFADADamyloid-β plaquemitochondrialNfLALSiPSCsorganoidsInhibitorinhibitorinhibit

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