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.
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- CAS. Nr.: 13422-16-7
- Formel: C13H9F3N2O2
- Molecular Weight:282.22
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
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Animal Model:Wistar (male, 230-260 g)[2]
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Dosage:10 mg/kg; 25 mg/kg; 50 mg/kg; 100 mg/kg; 200 mg/kg; 400 mg/kg
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Administration:p.o.; single dose
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Result:Produced significant hypoglycemia at 400 mg/kg at 2, 4, and 6 hours post-administration (97 mg/100 mL, 103 mg/100 mL, 109 mg/100 mL respectively; p < .05 vs. control).
Produced significant hyperglycemia at 50 mg/kg at 4 hours post-administration (120 mg/100 mL; p < .05 vs. control).
Produced significant hypoglycemia at 10 mg/kg at 6 hours post-administration (105 mg/100 mL; p < .05 vs. control).
Caused no significant blood glucose changes with 25 mg/kg, 100 mg/kg, or 200 mg/kg doses at any time point.
Chemical Information
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CAS. Nr. 13422-16-7
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Molecular Weight 282.22
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Formel C13H9F3N2O2
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SMILES
O=C(C1=C(NC2=CC=CC(C(F)(F)F)=C2)C=CN=C1)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Triflocin Related Classifications
HY-182386 Related Classifications
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