2. Membrane Transporter/Ion Channel
  3. Monoamine Transporter
  4. F3288-0031

F3288-0031 是一种去甲肾上腺素转运体 (NET) 变构抑制剂，在 20 µM 浓度下抑制率为 73.5%。F3288-0031 结合于 NET 的内腔稳定其内开口状态并对 NET/SERT 具有优先抑制活性其 pIC50 为 5.9。F3288-0031 未检测到脱靶功能活性。F3288-0031 表现出显著的抗抑郁样疗效且不伴有运动功能干扰。F3288-0031 可用于抑郁症及相关神经精神疾病的研究。

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F3288-0031

F3288-0031 Chemical Structure

CAS No. : 926493-93-8

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F3288-0031 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferential NET/SERT inhibition with pIC50 = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions[1].

体内研究
(In Vivo)

F3288-0031 (3-50 mg/kg，腹腔注射，单次给药) 在 C57BL/6J 小鼠中表现出抗抑郁样活性，且无运动活性干扰效应[1]。

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

Animal Model: Male C57BL/6J mice (6-8 weeks)[1]
Dosage: 3, 10, 30, 50 mg/kg
Administration: i.p., once
Result: Demonstrated a dose-dependent decrease in immobility time in the forced swim test (FST), with significant reductions at 30 and 50 mg/kg.
Did not significantly alter spontaneous locomotor activity at 3, 10, 30 mg/kg.
分子量

396.52

Formula

C24H32N2O3
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

F3288-0031 相关分类

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Keywords:

F3288-0031926493-93-8Monoamine TransporterNETNET/SERTdepressive disorderInhibitorinhibitorinhibit

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