Triflocin 

Triflocin is an orally active diuretic and Na⁺-K⁺-2Cl⁻ cotransporter inhibitor with an IC₅₀ of 3×10^-5 M. Triflocin inhibits the outward basolateral electrogenic Na-(HCO3) n>1 cotransport in the proximal tubule. Triflocin has no tendency to induce hyperglycemia, and its blood glucose-elevating effect is extremely weak, such that an increase in blood glucose levels can only be detected under special conditions such as glucose loading. Triflocin is more prone to induce hypoglycemia^[1][2].

Triflocin inhibits Na-K-2Cl cotransport in the thick ascending limb, with an IC₅₀ value of 3 × 10^-5 M^[1].
Triflocin has no effect on intracellular chloride ion activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Triflocin (10-400 mg/kg; p.o.; single administration) exerts dose-dependent effects on blood glucose in non-fasted male Wistar rats, causing significant hypoglycemia at 10 mg/kg (6-hour time point) and 400 mg/kg (2, 4, 6-hour time points), and significant hyperglycemia at 50 mg/kg (4-hour time point)^[2].
Triflocin (10-400 mg/kg; p.o.; single dose; 2 h before glucose loading) induces hypoglycemia in fasted male Wistar rats at doses of 50 mg/kg, 100 mg/kg and 400 mg/kg, and delays the onset of hyperglycemia at the dose of 400 mg/kg^[2].
Triflocin (100-400 mg/kg; subcutaneous injection; single administration; given 2 hours before glucose loading or immediately at glucose loading) induces hypoglycemia in fasted male Wistar rats during the oral glucose tolerance test, while delayed hyperglycemia occurs only at a dose of 400 mg/kg administered 2 hours before glucose loading^[2].
Triflocin (100-400 mg/kg; p.o.; daily; for 15 consecutive days) induces hypoglycemia at both 100 mg/kg and 400 mg/kg doses in the oral glucose tolerance test performed on fasted male Wistar rats, while only the 400 mg/kg dose causes delayed hyperglycemia^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

282.22

C₁₃H₉F₃N₂O₂

13422-16-7

O=C(C1=C(NC2=CC=CC(C(F)(F)F)=C2)C=CN=C1)O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Belachgar F, et al. Triflocin, a novel inhibitor for the Na-HCO3 symport in the proximal tubule. Br J Pharmacol. 1994 Jun;112(2):465-70.

  [2]. Gussin RZ, et al. The effect of a new diuretic, triflocin (4-(alpha,alpha,alpha-trifluoro-m-toluidino)-nicotinic acid) on blood glucose in the rat and dog. Proc Soc Exp Biol Med. 1969 Sep;131(4):1258-62.