他尼氟酯

Description

Talniflumate · CAS 66898-62-2 · C21H13F3N2O4. UNII JFK78S0U9S. Boiling Point: 454; Melting Point: 177; LogP: 4.47.

Identification

CAS Registry Number	66898-62-2
PubChem CID	48229
Molecular formula	C21H13F3N2O4
IUPAC name	(3-oxo-1H-2-benzofuran-1-yl) 2-[3-(trifluoromethyl)anilino]pyridine-3-carboxylate
UNII (FDA)	JFK78S0U9S

Computed Descriptors

Molecular Weight	414.3
XLogP3	5.3
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	5
Exact Mass	414.08274139
Monoisotopic Mass	414.08274139
Topological Polar Surface Area	77.5
Heavy Atom Count	30
Formal Charge	0

Physical & Chemical Properties

Boiling Point	454
Melting Point	177
LogP	4.47

Physical description & handling notes

• Talniflumate is metabolized to its prodrug, niflumic acid, which has several pharmacodynamic effects. Firstly, it blocks synthesis of mucin. Secondly, talniflumate blocks prostaglandin synthesis by cyclooxygenases, which aids in pain and inflammation management.

Documented Uses

• Talnifumate is a phthalidyl ester of nifumic acid, which has potent analgesic and anti-inflammatory effects and is widely used to treat inflammatory disorders, such as rheumatoid arthritis and osteoarthritis, and has also been studied for the management of cystic fibrosis.
• In 12 subjects after a single oral administration, total plasma clearance of the main metabolite, niflumic acid, averaged 45 ml/min giving a distribution volume of 0.12 l/kg on average.
• This drug undergoes extensive first pass effect.
• Niflumic acid, the active form of Talniflumate, is weak acid that is strongly bound to plasma proteins. Bioavailability was 100% in a study of 12 volunteers. It is a weak acid, strongly bound to plasma proteins.
• Approximately 2h in 12 subjects
• Talniflumate is a strong and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase). Talniflumate decreases gene expression of GCNT3 and production of mucins in vivo and in vitro. Talniflumate improves response of pancreatic tumors to gefitinib (chemotherapy drug). Talniflumate is a strong calcium-activated chloride channel (CaCC) blocker.

Synonyms

Talniflumate; 66898-62-2; Somalgen; Talniflumato; BA 7602-06; Talniflumatum; DTXSID3046740; Ba-7602-06; JFK78S0U9S; DTXCID1026740; RefChem:891040; 3-oxo-1,3-dihydro-2-benzofuran-1-yl 2-((3-(trifluoromethyl)phenyl)amino)pyridine-3-carboxylate; Lomucin; Talniflumatum [INN-Latin]; UNII-JFK78S0U9S; 3-Oxo-1,3-dihydroisobenzofuran-1-yl 2-((3-(trifluoromethyl)phenyl)amino)nicotinate

Frequently Asked Questions

What are the CAS number and molecular formula of Talniflumate?

CAS 66898-62-2; molecular formula C21H13F3N2O4; molecular weight — g/mol.

What other names is Talniflumate known by?

Talniflumate, 66898-62-2, Somalgen, Talniflumato, BA 7602-06, Talniflumatum.

What are the key physical properties of Talniflumate?

Boiling Point: 454; Melting Point: 177; LogP: 4.47.

Facts on this page are taken from PubChem (US National Library of Medicine) and Wikidata. Grade-specific data — assay, moisture, particle size, packaging, shelf life — is issued per batch on the COA and is not published here.