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

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.

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sEH inhibitor-20 Chemical Structure

sEH inhibitor-20 Chemical Structure

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Description

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].

In Vitro

sEH inhibitor-20 (Compound FP9) (0.1 μM, 1 h) shows excellent metabolic stability (t₁/₂ > 184 min) in human and mouse liver microsomes, indicating that it is not easily metabolized by the liver in vivo[1].
sEH inhibitor-20 (10 μM, 16 h) shows moderate brain permeability in the PAMPA-BBB model (Pe : 3.83 × 10⁻⁶ cm/s)[1].
sEH inhibitor-20 (1-1000 nM, pre-treat for 0.5 h, then treat for 6 h) significantly reduces TNF-α and IL-6 levels in the LPS-induced PBMC inflammation model without cytotoxicity (10 μM still does not affect cell survival)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 2 mg/kg i.v. T1/2 3.21 hr
Mice 10 mg/kg p.o. F 78 %
Mice 2 mg/kg i.v. MRT 3.50 hr
Mice 10 mg/kg p.o. T1/2 2.43 hr
Mice 2 mg/kg i.v. Vss 1.02 L/kg
Mice 10 mg/kg p.o. MRT 5.23 hr
Mice 2 mg/kg i.v. CL 4.80 mL/min/kg
Mice 10 mg/kg p.o. Cmax 4697 ng/mL
Mice 2 mg/kg i.v. Cmin 4642 ng/mL
Mice 10 mg/kg p.o. AUC0-inf 29708 ng·h/mL
Mice 2 mg/kg i.v. AUC0-inf 7631 ng·h/mL
In Vivo

sEH inhibitor-20 (Compound FP9) (10, 30 mg/kg, p.o.) has a potent and long-lasting analgesic effect in a Paclitaxel (HY-B0015) -induced neuropathic pain model and is not prone to tolerance[1].

MedChemExpress (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.
Molecular Weight

404.34

Formula

C19H15F3N4O3
SMILES

O=C1NN=C(C2=CC=C(NC(NCC3=CC=CC=C3OC(F)(F)F)=O)C=C2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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sEH inhibitor-20 Related Classifications

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Keywords:

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

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