2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Arrestin
  4. MW073

MW073 是一种高选择性、口服有效的 5-HT2BR 拮抗剂 (IC50 = 70 nM)。MW073 通过浓度依赖性地抑制受体活性和 β-arrestin-1 募集发挥作用。MW073 可改善阿尔茨海默病 (AD) 小鼠模型的突触可塑性和行为缺陷，包括攻击行为。MW073 可用于阿尔茨海默病相关研究[1][2]。

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MW073

MW073 Chemical Structure

CAS No. : 3048608-87-0

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MW073 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].

IC50 & Target[1]

5-HT2B Receptor

70 nM (IC50)

体外研究
(In Vitro)

MW073 (0.1-10 μM) 在转染的 HEK293A 细胞中对 h5-HT2BR (Kd = 86 nM, EC50Gprotein = 1.1 μM, EC50β-Arrestin1 = 2.4 μM) 和 m5-HT2BR (Kd = 125 nM, EC50Gprotein = 6.7 μM, EC50β-Arrestin1 = 0.6 μM) 的生化作用机制均为对血清素激发的受体激活、β-arrestin-1 招募以及基础构成性活性的剂量依赖性抑制，提示其具有反向激动剂潜力[1]。
MW073 在对 165 种不同 G 蛋白偶联受体进行的大规模细胞筛选中 (使用稳转 CHO 细胞系)，仅表现出对 5-HT2BR 的拮抗活性，而未显示其他受体激动或拮抗作用[1]。
MW073 对激酶、关键酶或转运体均无抑制活性，且其非 CYP450 酶底物的特性预示其具有较低的药物相互作用风险[1]。

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

MW073 相关抗体:
体内研究
(In Vivo)

MW073 (5 mg/kg， 腹腔注射，试验前 30 分钟) 能迅速挽救由 Aβ 或 Tau 寡聚体在 C57BL/6J 小鼠中诱导的急性突触可塑性与记忆缺陷[1]。
MW073 (0-5 mg/kg，口服，每日一次，从 60-70 日龄开始，持续 30-45 天) 剂量依赖性地预防和改善 APP/PS1 小鼠的记忆缺陷[1]。
MW073 (5 mg/kg，口服，每日一次，持续约 150-250 天) 可恢复 hTau/Mapt-KO 小鼠的突触和记忆功能，在慢性治疗期间的预防和治疗干预模式下均被证明有效[1]。
MW073 (5 mg/kg，腹腔注射，每日一次，持续 3 周) 可减少 Tg2576 小鼠的攻击性行为，且不会引发镇静或活动力低下的副作用[2]。

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

Animal Model: C57BL/6J mice (3-4 months old) infused with 200 nM Aβ- or 500 nM tau-oligomers or vehicle (intrahippocampal, 20 min prior to test)[1]
Dosage: 5 mg/kg
Administration: i.p., 30 min prior to test
Result: Attenuates both Aβ- and tau-oligomer-induced synaptic dysfunction.
Rescued long-term potentiation (LTP) deficit in hippocampal slices treated with Aβ or tau oligomers (perfused at 1.9 µM).Reduced errors in the 2-day radial arm water maze (RAWM) induced by Aβ or tau oligomers.
Attenuated both Aβ- and tau-oligomer–induced reduction in freezing in the contextual fear conditioning (FC).
Animal Model: hTau/Mapt-KO mice (7 months old)[1]
Dosage: 5 mg/kg
Administration: p.o., q.d. for ~250 days (prior to significant pathology)
Result: Prevented the impairment of LTP.
Re-established the normal number of errors in the RAWM (~180 days).
Protected against the impairment of associative memory in contextual FC (~240 days).
Animal Model: APP/PS1 transgenic mice (3-4 months old)[1]
Dosage: 0-5 mg/kg
Administration: p.o., q.d. for 30-45 days starting at the age of day 60-70
Result: Dose-dependently reduced the number of errors in the radial arm water maze (RAWM).
Ameliorated the contextual FC defect in a dose-dependent manner.
ED50 for RAWM improvement was 1.886 mg/kg.
Animal Model: hTau/Mapt-KO mice (11 months old)[1]
Dosage: 0-5 mg/kg
Administration: p.o, q.d. for ~150 days (after pathology onset)
Result: Restored the capability of undergoing LTP.
Protected against the impairment of spatial memory in the RAWM (~45 days).
Protected against the impairment of associative memory in contextual FC (~140 days).
Animal Model: Male Tg2576 mice[2]
Dosage: 5 mg/kg
Administration: i.p., q.d. for 3 weeks
Result: Significantly reduced aggressive behavior compared to the vehicle control group in the resident-intruder test.
Decreased the duration of the first attack.
Decreased the number of attacks and the total attack time.
Revealed no significant differences in the time spent in the center versus the periphery of the arena, number of entries into the center, and total distance traveled.
Did not alter locomotor function, anxiety-like behavior, or exploratory activity.
分子量

361.48

Formula

C22H27N5
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

MW073 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:

MW0733048608-87-0MW 073MW-0735-HT ReceptorArrestinSerotonin Receptor5-hydroxytryptamine Receptor5-HT2BRβ-arrestin-1AβtauADhTau/Mapt-KO miceAPP/PS1 miceTg2576Inhibitorinhibitorinhibit

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