2. Cytoskeleton
  3. Myosin
  4. MT-228

MT-228 (BPN-0026709) 是一种选择性且具有血脑屏障通透性的非肌肉肌球蛋白 II (non-muscle myosin II) 抑制剂。 MT-228 通过选择性靶向非肌肉肌球蛋白 II (non-muscle myosin II) (KI = 1.5 μM) 而非心脏肌球蛋白 II (CMII) (Ki = 17 μM) 显著改善了耐受性，并且 SmMll MD 的序列与 NMllB 的序列有 83.6% 的一致性。MT-228 在精神活性物质使用障碍的动物模型中显示出持久的效果。

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MT-228

MT-228 Chemical Structure

CAS No. : 2404652-24-8

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MT-228 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

MT-228 (BPN-0026709) is a selective and blood-brain barrier permeable non-muscle myosin II inhibitor. MT-228 markedly improves tolerability by selectively targeting NMIIB (KI = 1.5 μM) over CMII (KI = 17 μM), and the sequence of SmMll MD is 83.6% identical to that of NMllB. MT-228 shows long-lasting efficacy in animal models of stimulant use disorder[1].

体外研究
(In Vitro)

MT-228 (10-3-100 μM) 在 ATPase 实验中显示出比 Blebbistatin (HY-13813) 更高的心脏安全性和选择性，其 KINMIIB 值为 1.5 μM[1]。
MT-228 在细胞分裂抑制方面表现出优异的效果 (EC50 = 1.0 μM)[1]。

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

MT-228 相关抗体:
体内研究
(In Vivo)

MT 228 (5-10 mg/kg，腹腔注射，单次给药) 在小鼠中至少高达 10 mg/kg 时耐受性良好[1]。
MT-228 (0.5-5 mg/kg，腹腔注射或静脉注射，单次给药) 在小鼠和大鼠中破坏对兴奋活性物质的动机依赖[1]。

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

Animal Model: 8-10-week-old male C57BL/6 mice (25-30 g)[1]
Dosage: i.p. for a single dose
Administration: 5, 7.5, 10 mg/kg
Result: Showed no significant effects on distance travelled over the first 10 minutes or entire 40 minutes test period post-injection.
Showed no effect on velocity and no difference between time spent in the center versus the sides of the open field.
Animal Model: 8-10-week-old male C57BL/6 mice (25-30 g)[1]
Dosage: i.p. for a single dose
Administration: 0.5, 1, 2.5, 5 mg/kg
Result: Disrupted the motivation for METH at doses as low as 0.5 mg/kg.
Had no effect on a strong preference for the COC-paired chamber (5 mg/kg).
Had no effect on any measure in elevated plus maze, including the total distance travelled in the maze, latency to enter the open (unprotected) arm, or time spent in the open arm(5 mg/kg).
Animal Model: Adult male 250-300 g rats[1]
Dosage: i.v. for a single dose 30 minutes before testing
Administration: 1 mg/kg
Result: Reduced the robust lever pressing displayed by rats.
Removed the motivation to seek METH for at least one month.
分子量

337.37

Formula

C19H19N3O3
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

MT-228 相关分类

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  • 稀释计算器

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Keywords:

MT-2282404652-24-8BPN-0026709MT228MT 228BPN0026709BPN 0026709Myosinnon-muscle myosin IIstimulant use disorderInhibitorinhibitorinhibit

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MT-228
目录号：
HY-175199
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