An inhibitor of TMEM16A channels
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T16A(inh)-A01

Item No. 18518

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(5-ethyl-1,6-dihydro-4-methyl-6-oxo-2-pyrimidinyl)thio]-N-[4-(4-methoxyphenyl)-2-thiazolyl]-acetamide
CAS Number
552309-42-9
Molecular Formula
C19H20N4O3S2
Formula Weight
416.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2); (1:7): 0.1 mg/mlDMSO: 5 mg/ml
λmax
246, 274 nm
SMILES
COC1=CC=C(C2=CSC(NC(CSC(NC(C)=C3CC)=NC3=O)=O)=N2)C=C1
InChi Code
InChI=1S/C19H20N4O3S2/c1-4-14-11(2)20-18(23-17(14)25)28-10-16(24)22-19-21-15(9-27-19)12-5-7-13(26-3)8-6-12/h5-9H,4,10H2,1-3H3,(H,20,23,25)(H,21,22,24)
InChi Key
QSIYTNYMBWYHAA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $36

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    50 mg

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    Cayman Chemical
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    Product Description

    T16A(inh)-A01 is an aminophenylthiazole that inhibits transient TMEM16A-mediated chloride currents with an IC50 value of ~1 µM.1,2 Its inhibitory effects are independent of voltage and do not prolong the rate of TMEM16A current deactivation.2 T16A(inh)-A01 blocks CaCC activity in vascular smooth muscle cells and relaxes mouse and human blood vessels.3 It also inhibits the proliferation of pancreatic cancer and squamous carcinoma cells in culture.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Namkung, W., Phuan, P.W., and Verkman, A.S. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. The Journal of Biological Chemisty 286(3), 2365-2374 (2011).

    2. Bradley, E., Fedigan, S., Webb, T., et al. Pharmacological characterization of TMEM16A currents. Channels 8(4), 308-320 (2014).

    3. Davis, A.J., Shi, J., Pritchard, H.A.T., et al. Potent vasorelaxant activity of the TMEM16A inhibitor T16Ainh-A01. Br. J. Pharmacol. 168, 773-784 (2013).

    4. Mazzone, A., Eisenman, S.T., Strege, P.R., et al. Inhibition of cell proliferation by a selective inhibitor of the Ca2+ activated Cl- channel, Ano1. Biochem. Biophys. Res. Commun. 427(2), 248-253 (2012).

    5. Duvvuri, U., Shiwarski, D.J., Xiao, D., et al. TMEM16A induces MAPK and contributes directly to tumorigenesis and cancer progression. Cancer Res. 72(13), 3270-3281 (2012).