Tifenazoxide - 10mM in DMSO , CAS No.279215-43-9

CAS: 279215-43-9 Cat. No.: T655178 Molecular Weight: 291.78 PubChem CID: 135410911

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP 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

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. The EC 50 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. Tifenazoxide is a potent inhibitor of glucose stimulated insulin release from βTC6 cells (IC 50 = 0.15 µM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Vancouver diabetic fatty (VDF) Zucker rat 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.

IC50& Target:K ATP channels

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP 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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: CC1(CC1)N=C2NC3=C(SC(=C3)Cl)S(=O)(=O)N2
• WGK Germany: 3
• PubChem CID: 135410911
• Molecular Weight: 291.78