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T16Ainh-A01

  Cat. No.:  DC21956   Featured
Chemical Structure
552309-42-9
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Field of application
T16Ainh-A01 is an inhibitor of the calcium-activated chloride channel TMEM16A, inhibits Ca2+-activated Cl− channel (CACC) activity in TMEM16A-transfected FRT cells with IC50 of 1 uM; T16Ainh-A01 (1-30 uM) inhibited single calcium (Ca2+)-activated chloride (Cl−) channels and whole cell currents activated by 500 nM free Ca2+; T16Ainh-A01 relaxed mouse thoracic aorta pre-contracted with methoxamine with an IC50 of 1.6 uM and suppressed the methoxamine concentration-effect curve; blocks calcium-activated chloride channels in vascular smooth muscle cells and relaxes murine and human blood vessels.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 552309-42-9
Chemical Name: 2-[(5-Ethyl-1,6-dihydro-4-methyl-6-oxo-2-pyrimidinyl)thio]-N-[4-(4-methoxyphenyl)-2-thiazolyl]acetamide
Synonyms: T16Ainh-A01|
SMILES: COC1C=CC(C2=CSC(NC(CSC3NC(C)=C(CC)C(=O)N=3)=O)=N2)=CC=1
Formula: C19H20N4O3S2
M.Wt: 416.514
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Davis AJ, et al. Br J Pharmacol. 2013 Feb;168(3):773-84. 2. Mazzone A, et al. Biochem Biophys Res Commun. 2012 Oct 19;427(2):248-53. 3. Forrest AS, Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1229-43. 4. Namkung W, et al. J Biol Chem. 2011 Jan 21;286(3):2365-74.
Description: T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC)[1][2].
Target: TMEM16A[1].
References: [1]. Fedigan S, et al. Effects of new-generation TMEM16A inhibitors on calcium-activated chloride currents in rabbit urethral interstitial cells of Cajal. Pflugers Arch. 2017 Nov;469(11):1443-1455. [2]. Namkung W, et al. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. J Biol Chem. 2011 Jan 21;286(3):2365-74.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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