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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

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About This Item

Empirical Formula (Hill Notation):
C22H24N2O5S
CAS Number:
461000-66-8
Molecular Weight:
428.50
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD03115431
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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