2. Metabolic Enzyme/Protease
  3. Epoxide Hydrolase
  4. sEH inhibitor-20

sEH inhibitor-20 是一种代谢稳定具有口服活性的 sEH 抑制剂(IC50: 0.2 nM)。sEH inhibitor-20 具有显著的镇痛和抗炎活性，有望成为研究神经病理性疼痛的潜在候选化合物。

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sEH inhibitor-20

sEH inhibitor-20 Chemical Structure

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sEH inhibitor-20 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

sEH inhibitor-20 is an orally active and metabolically stable sEH inhibitor (IC50: 0.2 nM). sEH inhibitor-20 has significant analgesic and anti-inflammatory activities and is expected to become a potential candidate compound for the study of neuropathic pain[1].

体外研究
(In Vitro)

sEH inhibitor-20 (Compound FP9) (0.1 μM, 1 h) 在人和小鼠肝微粒体中，显示出优异的代谢稳定性 (t₁/₂ > 184 min)， 表明其在体内不易被肝脏快速代谢[1]。
sEH inhibitor-20 (10 μM, 16 h) 在 PAMPA-BBB 模型中，表现出中等程度的脑渗透性 (Pe : 3.83 × 10⁻⁶ cm/s)[1]。
sEH inhibitor-20 (1-1000 nM, 预处理 0.5 小时, 然后处理 6 小时) 在 LPS 诱导的 PBMC 炎症模型中，显著降低 TNF-α 和 IL-6 水平，无细胞毒性 (10 μM 时仍不影响细胞存活)[1]。

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

sEH inhibitor-20 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 10 mg/kg p.o. F 78 %
Mice 2 mg/kg i.v. T1/2 3.21 hr
Mice 10 mg/kg p.o. T1/2 2.43 hr
Mice 2 mg/kg i.v. MRT 3.50 hr
Mice 10 mg/kg p.o. MRT 5.23 hr
Mice 2 mg/kg i.v. Vss 1.02 L/kg
Mice 10 mg/kg p.o. Cmax 4697 ng/mL
Mice 2 mg/kg i.v. CL 4.80 mL/min/kg
Mice 10 mg/kg p.o. AUC0-inf 29708 ng·h/mL
Mice 2 mg/kg i.v. Cmin 4642 ng/mL
Mice 2 mg/kg i.v. AUC0-inf 7631 ng·h/mL
体内研究
(In Vivo)

sEH inhibitor-20 (Compound FP9) (10, 30 mg/kg, p.o.) 在紫杉醇 (HY-B0015) 诱导的神经病理性疼痛模型中具有强效且持久的镇痛作用，且不易产生耐受性[1]。

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

Animal Model: C57BL/6 mice (male, aged 6-8 weeks) intraperitoneally injected with Paclitaxel (5 mg/mL)[1]
Dosage: 10, 30 mg/kg
Administration: acute : p.o. one dose; chronic : p.o. once a day for 14 consecutive days
Result: Exhibited its maximum acute analgesic effect at 2 hours post-administration (30 mg/kg), with the effect persisting for 4 hours, demonstrating both longer duration and superior efficacy compared to gabapentin.
Maintained stable chronic analgesic effects at 30 mg/kg without inducing tolerance.
分子量

404.34

Formula

C19H15F3N4O3
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

sEH inhibitor-20 相关分类

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  • 稀释计算器

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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:

sEH inhibitor-20sEH inhibitor20sEH inhibitor 20Epoxide HydrolasePainPaclitaxelCD-1 micePAMPA-BBBTNF-αIL-6C57BL/6 mice,analgesicanti-inflammatoryInhibitorinhibitorinhibit

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