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(e): TMEM16A Activator, Eact, ANO1 Activator, Eact, 3,4,5-trimethoxy-N-(2-methoxyethyl)-N-(4-phenylthiazol-2-yl)benzamide, TMEM16A Activator, Eact
• Empirische Formel (Hill-System): C₂₂H₂₄N₂O₅S
• CAS-Nummer: 461000-66-8
• Molekulargewicht: 428.50
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD03115431
• Assay: ≥98% (HPLC)
• Form: powder
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• 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
• SMILES string: [s]1c(nc(c1)c3ccccc3)N(CCOC)C(=O)c2cc(c(c(c2)OC)OC)OC
• InChI: 1S/C22H24N2O5S/c1-26-11-10-24(22-23-17(14-30-22)15-8-6-5-7-9-15)21(25)16-12-18(27-2)20(29-4)19(13-16)28-3/h5-9,12-14H,10-11H2,1-4H3
• InChI key: ZUXNHFFVQWADJL-UHFFFAOYSA-N

Beschreibung

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable