1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. COX Carbonic Anhydrase LOX-1
  3. COX-2-IN-30

COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.

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COX-2-IN-30 Chemical Structure

COX-2-IN-30 Chemical Structure

CAS No. : 1160498-08-7

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Description

COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect[1].

IC50 & Target[1]

COX-2

49 nM (IC50)

COX-1

10.4 μM (IC50)

hCA I

183.4 nM (Ki)

hCA II

81.4 nM (Ki)

hCA IX

38.4 nM (Ki)

hCA XII

21.6 nM (Ki)

5-LOX

2.4 μM (IC50)

In Vitro

COX-2-IN-30 (compound 7a) binds to hCA isoforms with Ki values of 183.4 nM (hCA I), 81.4 nM (hCA II), 38.4 nM (hCA IX), 21.6 nM (hCA XII), respectively[1].

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

In Vivo

COX-2-IN-30 (compound 7a) (10 mg/kg; po; single dose) exhibits analgesic activity, while it results a significant reduction in the number of writhing in mice[1].
COX-2-IN-30 (10 mg/kg; po; single dose) results a significant reduction of paw height in Carrageenan (HY-125474)-induced rat paw edema assay. And COX-2-IN-30 siginificantly decreases the levels of TNF-α and IL-1β[1].
COX-2-IN-30 (10 mg/kg; po; single dose)shows safety profile on the gastric tissues, in male albino rats[1].

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

Animal Model: Albino mice (25-30 g)[1]
Dosage: 10 mg/kg
Administration: PO; single dose; after one hour, 0.1 mL of 1 percent acetic acid in a volume of 0.1 mL/10 g body weight was used to produce writhing.
Result: Decreased the number of writhing responses of mouse conpared with control group.
Animal Model: Paw edema rat induced by Carrageenan (HY-125474)[1]
Dosage: 10 mg/kg
Administration: PO; single dose; after one hour, 0.1 mL of 1% carrageenan solution was injected in the left hind paw; measure inflammation height at 0, 1, 2, and 3 h
Result: Showed a significant reduction of paw height compared to control after 3 h.
Molecular Weight

384.41

Formula

C17H16N6O3S

CAS No.
SMILES

O=C(C1=C(N(N=C1)C2=CC=C(C=C2)S(N)(=O)=O)N)N/N=C/C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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Product Name:
COX-2-IN-30
Cat. No.:
HY-149269
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