Talniflumate (BA 7602-06)

Alias: BA7602-06BA 7602-06BA-7602-06
Cat No.:V8865 Purity: ≥98%
Talniflumate(BA -602-06), a prodrug of Niflumic acid, is a potent,orally bioactive and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2b-1,6 N-acetylglucosaminyltrans-ferase).
Talniflumate (BA 7602-06) Chemical Structure CAS No.: 66898-62-2
Product category: Chloride Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Talniflumate (BA -602-06), a prodrug of Niflumic acid, is a potent,orally bioactive and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2b-1,6 N-acetylglucosaminyltrans-ferase). Talniflumate is a Ca2+-activated Cl- channel (CaCC) blocker and has to be converted to the active form Niflumic acid in order to exert its effects. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.

Biological Activity I Assay Protocols (From Reference)
ln Vivo
Talniflumate (oral chow; 0.4 mg/g; 21 days) dramatically enhanced survival in CF mice from 26% to 77%. It does not alter crypt goblet cell populations or modify intestinal expression of mCLCA3 but tends to diminish crypt mucoid impaction [1].
Animal Protocol
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.
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H13F3N2O4
Molecular Weight
414.3341
CAS #
66898-62-2
SMILES
O=C(C1=CC=CN=C1NC2=CC=CC(C(F)(F)F)=C2)OC3OC(C4=C3C=CC=C4)=O
InChi Key
ANMLJLFWUCQGKZ-UHFFFAOYSA-N
InChi Code
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)
Chemical Name
2-[[3-(Trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic acid 1,3-dihydro-3-oxo-1-isobenzofuranyl ester
Synonyms
BA7602-06BA 7602-06BA-7602-06
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~62.5 mg/mL (~150.85 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4135 mL 12.0677 mL 24.1354 mL
5 mM 0.4827 mL 2.4135 mL 4.8271 mL
10 mM 0.2414 mL 1.2068 mL 2.4135 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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