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COX-2-IN-30
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Catalog No. T78705Cas No. 1160498-08-7
COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].
COX-2-IN-30
😃Good
Catalog No. T78705Cas No. 1160498-08-7
COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | Inquiry | 8-10 weeks | |
| 50 mg | Inquiry | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1]. |
| Targets&IC50 | CA II (human):81.4 nM (Ki), COX-2:49 nM, CA (human):183.4 nM (Ki), 5-LOX:2.4 μM, COX-1:10.4 μM, CA XII (human):21.6 nM (Ki), CA IX (human):38.4 nM (Ki) |
| In vitro | COX-2-IN-30 (Compound 7a) binds to human carbonic anhydrase (hCA) isozymes, with inhibitory constants (K i values) of 183.4 nM (hCA I), 81.4 nM (hCA II), 38.4 nM (hCA IX), and 21.6 nM (hCA XII) [1]. |
| In vivo | COX-2-IN-30, administered orally at 10 mg/kg, showed analgesic activity by significantly reducing writhing frequency in mice and decreased paw swelling in the carrageenan-induced rat paw edema test. It also significantly reduced pro-inflammatory cytokines TNF-α and IL-1β and demonstrated safety in the gastric tissues of male albino rats at the same dosage and administration method [1]. |
| Molecular Weight | 384.41 |
| Formula | C17H16N6O3S |
| Cas No. | 1160498-08-7 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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