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T16Ainh-A01

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Chemical Structure| 552309-42-9 同义名 : T16A(inh)-A01
CAS号 : 552309-42-9
货号 : A648561
分子式 : C19H20N4O3S2
纯度 : 98%+
分子量 : 416.517
MDL号 : MFCD03278952
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(204.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 10 mg/mL(24.01 mM)
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.00mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL
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