Talniflumate (BA 7602-06)   中文名称: 他尼氟酯

他尼氟酯（口服食物；0.4 毫克/克；21 天）可将 CF 小鼠的存活率从 26% 显着提高至 77%。它不会改变隐窝杯状细胞群或改变 mCLCA3 的肠道表达，但往往会减少隐窝粘液嵌塞 [1]。

Animal/Disease Models: CF mice with distal intestinal obstruction syndrome (DIOS)[1]
Doses: 0.4 mg/g
Route of Administration: oral; 21-day
Experimental Results: Distal intestinal obstruction syndrome cystic fibrosis mouse model The survival rate is improved.

Absorption, Distribution and Excretion
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.

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Metabolism / Metabolites
Extensive liver metabolism.

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Biological Half-Life
Approximately 2h in 12 subjects

Protein Binding
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.

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

[2]. 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.

2-[3-(trifluoromethyl)anilino]-3-pyridinecarboxylic acid (3-oxo-1H-isobenzofuran-1-yl) ester is a member of benzofurans.
Talniflumate, is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma. In addition, it is used in inflammatory conditions such as rheumatoid arthritis. Phase I trials with talniflumate for the treatment of cystic fibrosis and COPD were completed in August 2001, and phase II trials were performed in Ireland for the treatment of cystic fibrosis but this research has now been discontinued. Talniflumate has been approved for approximately 20 years in Argentina other countries (excluding the United States, Europe, and Japan).

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Drug Indication
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.

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Mechanism of Action
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.

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Pharmacodynamics
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.

C21H13F3N2O4

414.3341

414.082

66898-62-2

48229

White to yellow solid powder

1.5±0.1 g/cm3

534.6±50.0 °C at 760 mmHg

165-167ºC

277.1±30.1 °C

0.0±1.4 mmHg at 25°C

1.625

5.59

77.52

1

9

5

30

644

0

FC(C1C([H])=C([H])C([H])=C(C=1[H])N([H])C1=C(C([H])=C([H])C([H])=N1)C(=O)OC1([H])C2=C([H])C([H])=C([H])C([H])=C2C(=O)O1)(F)F

ANMLJLFWUCQGKZ-UHFFFAOYSA-N

InChI=1S/C21H13F3N2O4/c22-21(23,24)12-5-3-6-13(11-12)26-17-16(9-4-10-25-17)19(28)30-20-15-8-2-1-7-14(15)18(27)29-20/h1-11,20H,(H,25,26)

2-[[3-(Trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic acid 1,3-dihydro-3-oxo-1-isobenzofuranyl ester

BA7602-06BA 7602-06BA-7602-06

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~62.5 mg/mL (~150.85 mM)

配方 1 中的溶解度: ≥ 2.08 mg/mL (5.02 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。