Top Suppliers:I want be here
Hot CAS#:
56-41-7 108-65-6
56-35-9 64-17-5
67-56-1 108-88-3
141-78-6 1310-73-2
13463-67-7 1333-86-4

279215-43-9

279215-43-9 structure
279215-43-9 structure
  • Name: Tifenazoxide
  • Chemical Name: 2H-Thieno(3,2-E)-1,2,4-thiadiazin-3-amine, 6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide
  • CAS Number: 279215-43-9
  • Molecular Formula: C9H10ClN3O2S2
  • Molecular Weight: 291.77800
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
  • Create Date: 2017-10-06 17:06:18
  • Modify Date: 2024-01-15 11:43:48
  • Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis[1][2].
Name 2H-Thieno(3,2-E)-1,2,4-thiadiazin-3-amine, 6-chloro-N-(1-methylcyclopropyl)-, 1,1-dioxide
Description Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis[1][2].
Related Catalog
Target

KATP channels[1][2]

In Vitro Tifenazoxide (NN414) hyperpolarises βTC3 cell membranes, and inhibits insulin release from βTC6, from isolated rat islets and from human islets at least a 100-fold more potent than Diazoxide[2]. The EC50 values for Tifenazoxide and diazoxide are 0.45 and 31 µM, respectively in the patch-clamp assay. Tifenazoxide (100 µM) activates Kir6.2/SUR1 channels, but not Kir6.2/SUR2A or Kir6.2/SUR2 channels, expressed in Xenopus oocytes both in whole-cell and inside-out macropatch recordings[2]. Tifenazoxide is a potent inhibitor of glucose stimulated insulin release from βTC6 cells (IC50 = 0.15 µM)[1].
In Vivo Tifenazoxide (NN414; 1.5 mg/kg; oral administration; twice daily; for 3 weeks; male VDF Zucker (fa/fa) rat) treatment for 3 weeks in VDF rats reduces basal hyperglycemia, improves glucose tolerance, and reduces hyperinsulinemia during an oral glucose tolerance test (OGTT) and improves insulin secretory responsiveness ex vivo[1]. Animal Model: Male Vancouver diabetic fatty (VDF) Zucker rat[1] Dosage: 1.5 mg/kg Administration: Oral administration; twice daily; for 3 weeks Result: Basal glucose was significantly reduced with the fall averaging 0.64 mM after 3 weeks of treatment.
References

[1]. Carr RD, et al. NN414, a SUR1/Kir6.2-selective potassium channel opener, reduces blood glucose and improves glucose tolerance in the VDF Zucker rat. Diabetes. 2003 Oct;52(10):2513-8.

[2]. Hansen JB. Towards selective Kir6.2/SUR1 potassium channel openers, medicinal chemistry and therapeutic perspectives. Curr Med Chem. 2006;13(4):361-76.
Molecular Formula C9H10ClN3O2S2
Molecular Weight 291.77800
Exact Mass 290.99000
PSA 107.18000
LogP 3.05910
Vapour Pressure 3.22E-08mmHg at 25°C
RIDADR NONH for all modes of transport

Chemsrc provides CAS#:279215-43-9 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 279215-43-9 | Chemsrc address: https://www.chemsrc.com/en/baike/303690.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved