552309-42-9|2-((5-Ethyl-4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)thio)-N-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide|CsnPharm

CAS No.: 552309-42-9

T16Ainh-A01 Catalog No. CSN27627

Synonyms: T16A(inh)-A01

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).

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描述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). Depolarization-evoked I ClCa in isolated RUICC, recorded using voltage clamp, were inhibited by T16Ainh-A01 with IC50 values of 3.4 μM. Eurogenic contractions of strips of rabbit urethra smooth muscle (RUSM), evoked by electric field stimulation (EFS), were also significantly reduced by T16Ainh-A01^[1]. T16Ainh-A01 (10 μM) inhibits nearly completely TMEM16A chloride current (induced by 275 nM free calcium in the pipette) at all voltages, indicating a voltage-independent block mechanism^[2]. T16Ainh-A01 led to the significant repression of cell proliferation, cell migration, and collagen secretion in CFs(cardiac fibroblasts)^[3]. Suppression of ANO1 activity either by selective inhibitor (T16Ainh-A01) or by siRNA significantly attenuated the migration and invasion of ATC (Anaplastic thyroid carcinoma) cells^[4].
参考文献

[1] Fedigan S, Bradley E, Webb T, Large RJ, Hollywood MA, Thornbury KD, McHale NG, Sergeant GP. 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, Phuan PW, Verkman AS. 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
[3] Tian XQ, Ma KT, Wang XW, Wang Y, Guo ZK, Si JQ. Effects of the Calcium-Activated Chloride Channel Inhibitors T16Ainh-A01 and CaCCinh-A01 on Cardiac Fibroblast Function. Cell Physiol Biochem. 2018;49(2):706-716
[4] Kim JY, Youn HY, Choi J, Baek SK, Kwon SY, Eun BK, Park JY, Oh KH. Anoctamin-1 affects the migration and invasion of anaplastic thyroid carcinoma cells. Anim Cells Syst (Seoul). 2019 May 10;23(4):294-301

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4009 mL
- 12.0043 mL
- 24.0086 mL
- 5 mM
- 0.4802 mL
- 2.4009 mL
- 4.8017 mL
- 10 mM
- 0.2401 mL
- 1.2004 mL
- 2.4009 mL

技术信息

CAS号

552309-42-9

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H20N4O3S2

运输

蓝冰

分子量

416.52

别名

T16A(inh)-A01

溶解度

DMSO	83.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	Insoluble

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