Celecoxib CAS 169590-42-5 Pharmaceutical Raw Materials For Anti Inflammatory Treatment

Mechanisms of Action

Celecoxib has the anti-inflammatory and analgesic effect of NSAIDs. Because of its chemical structure, it can be combined with COX-2, selectively inhibiting COX-2. Its phenyl group binds with the hydrophobic channel of COX-2, and its hydrophilic sulfonamide forms a hydrogen chain with 513 arginine and 90 histidine in the COX-2 "side pocket.” It is also in close contact with arginine in the COX-2120 position and plays a role in inhibiting COX-2 from converting arachidonic acid to prostaglandins which are harmful to the human body. Due to subtle differences between the structures of COX-1 and COX-2, Celecoxib cannot enter the COX-1 molecule, nor inhibit its transformation of arachidonic acid into prostaglandins. Thus, it has good anti-inflammatory and analgesic effects, protects gastric mucosa, protects renal blood flow, regulates platelet aggregation, and resolves the gastric irritation problems of commonly used NSAIDs.

Indications and Usage

Celecoxib and Rofecoxib are two currently used COX-2 inhibitors. Successfully developed by GD Searle & Pfizer Co. (U.S.,) released in 1999, trade name: Celebrex.
Celecoxib is a nonsteroidal, anti-inflammatory agent with significant analgesic and anti-inflammatory effects, causing the lowest incidence of upper gastrointestinal tract ulcers and other complications. Used clinically to treat acute and chronic osteoarthritis and rheumatoid arthritis, with an anti-inflammatory analgesic role, relieving the signs and symptoms of osteoarthritis and rheumatoid arthritis.

Description

Celecoxib is a nonsteroidal antiinflammatory drug (NSAID) first launched as Celebrex in the US for the treatment of symptoms in patients with rheumatoid arthritis (RA) and osteoarthritis (OA). Celecoxib belongs to a new class of 1, 5-diarylpyrazoles and can be synthesized by heat-promoted heterocyclization of a trifiuoro-l,3-dione with appropriate arylhydrazine. Celecoxib is a highly selective inhibitor of COX-2, the inducible form of cyclooxygenase expressed during inflammatory processes; it does not block the constitutive form COX-1, thus suppressing the gastric and intestinal toxicity of most non-selective NSAIDs. The potency ratio COX1/COX2 on purified human enzymes was about 400. In several in vivo models of acute and chronic inflammation, Celecoxib demonstrated potent antiinflammatory activity without affecting gastric or urinary prostaglandin PGE2. In several clinical studies performed with patients suffering from osteoarthritis or rheumatoid arthritis, Celecoxib was shown to be well tolerated and to relieve pain and inflammation more efficiently compared with other standard NSAIDs; the gastrointestinal safety profile was significantly better than that of other NSAIDs. Interestingly, Celecoxib was approved for another indication in patients with familial adenomatous polyposis (FAP). A six-month clinical trial demonstrated a 28% reduction in the number of colorectal polyps with Celecoxib, compared to a 5% reduction with placebo

Uses

A selective cyclooxygenase-2 (COX-2) inhibitor. Anti-inflammatory. Used in treatment of familial adenomatous polyposis

For relief and management of osteoarthritis (OA), rheumatoid arthritis (RA), juvenile rheumatoid arthritis (JRA), ankylosing spondylitis, acute pain, primary dysmenorrhea and oral adjunct to usual care for patients with familial adenomatous polyposis

Product Description

Celecoxib Basic information

Indications and Usage Application in Particular Diseases Mechanisms of Action Pharmacokinetics Clinical Research Side Effects Warnings and Precautions

Product Name:	Celecoxib
Synonyms:	4-[5-(4-Methylphenyl)-3-trifluoromethyl)-1H-pyrazol-yl]benzenesulfonamide Celecoxib;CJ-016377;CP-598107;PF-00345549;PHA-00846533;Celecoxib Solution, 100ppm;Celecoxib (200 mg);Celocoxib, >=99%
CAS:	169590-42-5
MF:	C17H14F3N3O2S
MW:	381.37
EINECS:	685-962-5
Product Categories:	MONASIRUP;Pfizer compounds;Active Pharmaceutical Ingredients;All Inhibitors;Sulfur & Selenium Compounds;Celecoxib;Osteoarthritis and Rheumatoid Arthritis;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Stable Isotopes;API
Mol File:	169590-42-5.mol

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Lihe Pharm Technology (Wuhan) Co., Ltd. has a registered capital of 3 million yuan, and our products have a great price advantage in Europe and South America. We are an experienced manufacturer of various apis, pharmaceutical intermediates, organic and inorganic chemicals. We provide samples to test the quality as a trial order, because I have confidence in the quality of our products, many foreign customers, received our goods will be consistent praise.

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