613550

TMEM16A Activator, Eact

The TMEM16A Activator, Eact modulates the biological activity of TMEM16A. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• Synonym(s): TMEM16A Activator, Eact, ANO1 Activator, Eact, 3,4,5-trimethoxy-N-(2-methoxyethyl)-N-(4-phenylthiazol-2-yl)benzamide, TMEM16A Activator, Eact
• Empirical Formula (Hill Notation): C₂₂H₂₄N₂O₅S
• CAS Number: 461000-66-8
• Molecular Weight: 428.50
• MDL number: MFCD03115431
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL, clear, colorless
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

An N-aroylaminothiazole that strongly activates TMEM16A (ANO1) calcium-activated chloride channel (CaCC) at 0 Ca²⁺ concentration (Ca²⁺ independent), with the capability of producing large and sustained CaCC Cl-1 currents (EC₅₀ = 3 µM) in TMEM16A-expressing Fisher Rat Thyroid (FRT) Cells without elevation of cytoplasmic Ca2+ level, and in human A253 cells. Shown to increase CaCC conductance in human salivary and airway submucosal gland epithelial cells, IL-4 treated bronchial cells, and stimulated submucosal gland secretion in human bronchi and smooth muscle contraction in mouse intestine. Activation effect can be abolished by the addition of a TMEM16A inhibitor T16A-A01 at 10 µM in TMEM16A-transfected cells and in cultures of human salivary gland and IL-4-treated bronchial epithelia, but not in intestine. Does not affect CFTR Cl- conductance or ENaC Na+ conductance.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Namkung, W., et al. 2011. FASEB J.25, 4048.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable