2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Epoxide Hydrolase COX
  4. COX-2/sEH-IN-1

COX-2/sEH-IN-1 (Compound 9c) 是一种具有口服活性的 COX-2 和 sEH (可溶性环氧化物水解酶) 双抑制剂，对 COX-2 和 sEH 的 IC50 值分别为1.24 µM和0.40 nM。COX-2/sEH-IN-1 能提高抗炎活性、大大降低低心血管风险。

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COX-2/sEH-IN-1 Chemical Structure

COX-2/sEH-IN-1 Chemical Structure

CAS No. : 2474977-38-1

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COX-2/sEH-IN-1 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks[1].

IC50 & Target

COX-2

1.24 μM (IC50)

COX-1

8.72 μM (IC50)

sEH

0.40 nM (IC50)

体内研究
(In Vivo)

COX-2/sEH-IN-1 (Compound 9c) (10 mg/kg; p.o.; once) exhibits analgesic activity[1].
COX-2/sEH-IN-1 (50 mg/kg; p.o.; once) shows high anti-inflammatory activity[1].
COX-2/sEH-IN-1 (100 mg/kg; p.o.; 2 weeks) affords a perfect cardio-protection and less cardiovascular liabilities[1].

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

Animal Model: Albino mice (20-30 g)[1]
Dosage: 10 mg/kg
Administration: Oral administration, once
Result: Exhibited analgesic activity with 65.67% inhibition in the number of writhing.
Animal Model: Albino rats (120-150 g), carrageenan-induced paw edema model[1]
Dosage: 50 mg/kg
Administration: Oral administration, once
Result: Showed high anti-inflammatory activity with edema inhibition of 64.06%, 95.82%, and 98.15% at 1, 3, 5 h, respectively.
Animal Model: Adult male albino Wister rats (170-200 g)[1]
Dosage: 100 mg/kg
Administration: Oral administration, 2 weeks
Result: Exhibited a significant lowering in Troponine-I, LDH and CK-MB levels when compared to celecoxib treated group. Showed remarkably decrease in TNF-α concentration compared to the celecoxib induced cardio-toxicity group. Restored heart GSH level and significantly increased PGI2 level compared to celecoxib group. Showed mild decongestant and mild edema on cardiac blood vessels and showed more or less normal muscle bundles.
分子量

501.48

Formula

C23H18F3N5O3S
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

COX-2/sEH-IN-1 相关分类

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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:

COX-2/sEH-IN-12474977-38-1Epoxide HydrolaseCOXCyclooxygenaseAlbino miceAlbino ratsAnalgesic activityAnti-inflammatory activityCardiovascularTNF-αInhibitorinhibitorinhibit

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产品名称：
COX-2/sEH-IN-1
目录号：
HY-146704
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