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COX-2-IN-30

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

COX-2-IN-30

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].
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight384.41
FormulaC17H16N6O3S
Cas No.1160498-08-7
Storage & Solubility Information
StorageShipping with blue ice.

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