2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. ENX-101

ENX-101 是一种口服有效的 (GABAA) 受体部分正向变构调节剂 (PAM)。ENX-101 对 GABA 受体的 α2β2γ2L (EC50 = 0.76 nM)、α2β3γ2L (EC50 = 0.61 nM)、α3 (EC50 = 1.97 nM)、α5 (EC50 = 0.85 nM) 亚基具有选择性。ENX-101 在多种动物模型中表现出抗癫痫活性。

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ENX-101 Chemical Structure

ENX-101 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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ENX-101 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

ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models[1].

体外研究
(In Vitro)

ENX-101 (0.01 nM-10 μM) 能有效增强中国仓鼠卵巢 (CHO) 细胞中含有 α2、α3、α5 亚基的受体中由 GABA 产生的电流，但对含有 α1 亚基的受体的增强作用却微乎其微[1]。

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

ENX-101 相关抗体:
体内研究
(In Vivo)

ENX-101 (30-300 mg/mL，腹腔注射，在电流刺激前 0.25 小时单次给药) 在杂交成年雄性 CF-1 小鼠 (20-35 g) 模型中，可保护大多数在 32 mA 电流下受到刺激的动物，但在 44 mA 电流下保护较少的动物[1]。
ENX-101 (1-100 mg/kg，口服，在电刺激前 2 小时单次给药) 在癫痫大鼠模型中，以剂量依赖性方式显著抑制行为性癫痫发作反应，并缩短杏仁核和皮质的平均放电后持续时间[1]。
ENX-101 (0.075-100 mg/kg，口服，单剂量) 显著降低了雄性斯特拉斯堡 Wistar 遗传性失神癫痫大鼠 (GAERS) 在治疗后观察期 (10-130分钟) 内的整体棘波放电 (SWD)[1]。
ENX-101（10-100 mg/kg，口服，单剂量）在大鼠模型中，抗癫痫剂量未引起运动障碍[1]。

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

Animal Model: Amygdala kindled seizure rat model [1]
Dosage: 1 mg/kg, 6 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral gavage (p.o.)
Result: Significantly reduced the mean seizure severity score by -1.8 (p < 0.01), -3.2 (p < 0.001), -3.8 (p < 0.01) respectively.
Reduced mean afterdischarge duration in the cortex (−30%, p < 0.01; −53%, p < 0.01; and −66%, p < 0.001) and amygdala −26% (p < 0.01), −46% (p < 0.01), and −64% (p < 0.001).
Showed greatest reductions in seizure severity score (-4.0) and afterdischarge duration in the cortex (−76%, p < 0.05) and in the amygdala (−78%) with 100 mg/kg but without significance.
Resulted in average plasma exposures of 191, 487, and 1102 ng/mL 2 h after dosing with 1, 6, 30 mg/kg.
Clinical Trial
分子量

426.47

Formula

C19H12D9F2N7O2
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

ENX-101 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

ENX-101ENX101ENX 101GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα2α3α5selectiveGABAAreceptorPAMantiseizureInhibitorinhibitorinhibit

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