134729-13-8
134729-13-8 structure
- Name: COX2-IN-1
- Chemical Name: COX2-IN-1
- CAS Number: 134729-13-8
- Molecular Formula: C17H12FN3O2S
- Molecular Weight: 341.36
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2018-03-12 01:45:47
- Modify Date: 2025-08-26 19:29:44
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COX2-IN-1 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.
| Name | COX2-IN-1 |
|---|
| Description | COX2-IN-1 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities. |
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| Related Catalog | |
| Target |
COX-2:240 nM (IC50) |
| In Vitro | COX2-IN-1 shows no COX-1 inhibition even at 100μM[1]. |
| In Vivo | COX2-IN-1 has oral ED50 values of 0.030 and 0.47mg/kg on adjuvant-induced arthritis and collagen-induced arthritis, respectively, and an ED30 value of 7.4mg/kg in the yeast-induced hyperalgesia (Randall-Selitto) assay. COX2-IN-1 shows good analgesic activity and no ulcerogenicity[1]. |
| Kinase Assay | hCOX1 or hCOX2 is preincubated with COX2-IN-1 in 0.1 M Tris-HCl buffer containing 2 μM hematin and 5 mM L-tryptophan at 30 °C for 5 min, followed by a 5 min incubation with arachidonic acid. The enzyme reaction is stopped by the addition of 1 N HCl. The PGE2 formed is extracted with EtOAc and measured by RIA[1]. |
| Animal Admin | Rats: Ten male Sprague Dawley rats are used per group. A suspension of 0.5% brewer's yeast in 0.5% methyl cellulose is injected into the right hind paw. The pain threshold us determined 3h after yeast injection. COX2-IN-1 is given orally 2 h after yeast injection. The pain threshold in the treated rats are compared with that in the control rats[1]. |
| References |
| Molecular Formula | C17H12FN3O2S |
|---|---|
| Molecular Weight | 341.36 |