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Talniflumate

Names

[ CAS No. ]:
66898-62-2

[ Name ]:
Talniflumate

[Synonym ]:
3-oxo-1,3-dihydro-2-benzofuran-1-yl 2-{[3-(trifluoromethyl)phenyl]amino}pyridine-3-carboxylate
Talniflumate
2-[[3-(Trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic Acid 1,3-Dihydro-3-oxo-1-isobenzofuranyl Ester
Phthalidyl 2-(a,a,a-Trifluoro-m-toluidino)nicotinate
3-Pyridinecarboxylic acid, 2-[[3-(trifluoromethyl)phenyl]amino]-, 1,3-dihydro-3-oxo-1-isobenzofuranyl ester
Lomucin
Somalgen
Purotoxin 1
BA 7602-06
3-Oxo-1,3-dihydro-2-benzofuran-1-yl 2-{[3-(trifluoromethyl)phenyl]amino}nicotinate

Biological Activity

[Description]:

Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase[1]. Talniflumate is an orally active ca2+-activated Cl- channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome[2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Chloride Channel
Research Areas >> Inflammation/Immunology

[Target]

IC50: ca2+-activated Cl- channel (CaCC)[1]


[In Vivo]

Talniflumate (oral chow; 0.4 mg/g; 21 days) significantly increases CF mouse survival from 26 to 77%. It does not alter crypt goblet cell numbers or change intestinal expression of mCLCA3 but tends to decrease crypt mucoid impaction[1]. Animal Model: CF mice with distal intestinal obstructive syndrome (DIOS)[1] Dosage: 0.4 mg/g Administration: Oral chow; 21 days Result: Increased survival in a cystic fibrosis mouse model of distal intestinal obstructive syndrome.

[References]

[1]. Hyun-Ji Kim, et al. Pharmacokinetics of talniflumate, a prodrug of niflumic acid, following oral administration to man. Archives of Pharmacal Research volume 19, Article number: 297 (1996)

[2]. Mollereau, et al. Agonist and Antagonist Activities on Human NPFF(2) Receptors of the NPY Ligands GR231118 and BIBP3226. Br J Pharmacol.2001 May;133(1):1-4.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
534.6±50.0 °C at 760 mmHg

[ Melting Point ]:
165-167ºC

[ Molecular Formula ]:
C21H13F3N2O4

[ Molecular Weight ]:
414.334

[ Flash Point ]:
277.1±30.1 °C

[ Exact Mass ]:
414.082733

[ PSA ]:
77.52000

[ LogP ]:
5.59

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.625

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QT2999200
CHEMICAL NAME :
Nicotinic acid, 2-(alpha,alpha,alpha-trifluoro-m-toluidino)-, phthalidyl ester
CAS REGISTRY NUMBER :
66898-62-2
LAST UPDATED :
199612
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C21-H13-F3-N2-O4
MOLECULAR WEIGHT :
414.36
WISWESSER LINE NOTATION :
T56 BVO DHJ DOV- CT6NJ BMR CXFFF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
12 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 36,372,1981
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,448,1979
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>4 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,448,1979

Safety Information

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Related Compounds

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