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。
| 生物活性 | COX-2/sEH-IN-1 (Compound 9c) is an orally active, dualCOX-2andsEH(soluble epoxide hydrolase) inhibitor withIC50values of 1.24 μM and 0.40 nM againstCOX-2and 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) |
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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].
| 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. |
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| 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. |
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