T16Ainh - A01 |
Catalog No.GC17930
One-Click Copy Product Info
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T16Ainh - A01, un aminofeniltiazol, es un potente inhibidor de la proteína transmembrana 16A (TMEM16A), que inhibe las corrientes de cloruro mediadas por TMEM16A con un valor IC50 de ~1 µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 552309-42-9
Sample solution is provided at 25 µL, 10mM.
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T16Ainh - A01 is a potent transmembrane protein 16A (TMEM16A) inhibitor with an IC50 value of 1µM for inhibiting TMEM16A chloride current[1]. T16Ainh - A01 suppresses vascular contraction and promotes vasodilation by blocking calcium-activated chloride channels[2]. T16Ainh - A01 has been widely used to abolish Ca2+ transients in urethral smooth muscles and impede embryo implantation and decidualization[3-4].
In vitro, T16Ainh - A01 (10µM) treatment for 48 hours inhibited the expression of ANO1 and α-SMA mRNA in rat cardiac fibroblasts (CFs), suppressed collagen secretion, and induced cell cycle arrest[5]. Incubation with 20µM T16Ainh - A01 for 24 hours markedly reduced the proliferation of immortalized human pancreatic ductal epithelium cells (HPDECs) and altered the ATP-induced Ca2+ signal[6]. Treatment with 30µM T16Ainh - A01 for 72 hours reduced the growth of PC-3 cells and induced cell apoptosis, as well as promoting the expression and secretion of TNF-α[7].
In vivo, tail vein injection of T16Ainh - A01 at a dose of 0.33mg/kg every other day for 2 weeks alleviated pulmonary arteriolar remodeling and right ventricular hypertrophy, and inhibited the elevation of blood pressure in a rat model of pulmonary arterial hypertension (PAH)[8]. Topical application of 15µl of 100µM T16Ainh - A01 daily for 7 days alleviated imiquimod cream-induced psoriasis-like symptoms in mouse ears and reduced the expression of ANO1 and pERK1/2[9].
References:[1] Namkung W, Phuan P W, Verkman A S. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells[J]. Journal of Biological Chemistry, 2011, 286(3): 2365-2374.
[2] Davis A J, Shi J, Pritchard H A T, et al. Potent vasorelaxant activity of the TMEM16A inhibitor T16Ainh‐A01[J]. British journal of pharmacology, 2013, 168(3): 773-784.
[3] Fedigan S, Bradley E, Webb T, et al. Effects of new-generation TMEM16A inhibitors on calcium-activated chloride currents in rabbit urethral interstitial cells of Cajal[J]. Pflügers Archiv-European Journal of Physiology, 2017, 469(11): 1443-1455.
[4] Qi Q, Yang Y, Wu K, et al. Inhibition of TMEM16A impedes embryo implantation and decidualization in mice[J]. Reproduction, 2018, 156(6): 569-577.
[5] Tian X, Ma K, Wang X, et al. Effects of the calcium-activated chloride channel inhibitors T16Ainh-A01 and CaCCinh-A01 on cardiac fibroblast function[J]. Cellular Physiology and Biochemistry, 2018, 49(2): 706-716.
[6] Sauter D R P, Novak I, Pedersen S F, et al. ANO1 (TMEM16A) in pancreatic ductal adenocarcinoma (PDAC)[J]. Pflügers Archiv-European Journal of Physiology, 2015, 467(7): 1495-1508.
[7] Song Y, Gao J, Guan L, et al. Inhibition of ANO1/TMEM16A induces apoptosis in human prostate carcinoma cells by activating TNF-α signaling[J]. Cell death & disease, 2018, 9(6): 703.
[8] Xie J, Liu W, Lv W, et al. Transmembrane protein 16A/anoctamin 1 inhibitor T16Ainh-A01 reversed monocrotaline-induced rat pulmonary arterial hypertension[J]. Pulmonary Circulation, 2020, 10(4): 2045894020946670.
[9] Choi M R, Kim H D, Cho S, et al. Anoctamin1 induces hyperproliferation of HaCaT keratinocytes and triggers imiquimod-induced psoriasis-like skin injury in mice[J]. International journal of molecular sciences, 2021, 22(13): 7145.
| Cell experiment [1]: | |
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Cell lines |
A375 cells |
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Preparation Method |
A375 cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum (FBS), 100U/ml penicillin, and 100µg/ml streptomycin, at 37°C in an incubator with 5% CO2. Cells were inoculated at a density of 1000 cells/well into 96-well plates. 24h later, when the cells had adhered to the bottom of the plate, the cells were treated with different concentrations (0, 3, 10, 20, 30, and 50μM) of T16Ainh - A01. At 72h post-treatment, cell viability was measured. |
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Reaction Conditions |
0, 3, 10, 20, 30, and 50μM; 72h |
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Applications |
T16Ainh - A01 treatment reduced cell viability of A375 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague-Dawley rats |
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Preparation Method |
Male Sprague-Dawley rats (8 weeks old) were housed with a regular 12h light/dark cycle at a controlled temperature (23±1℃) and were given free access to food and water. To establish the PAH model, rats were intraperitoneally injected with 50mg/kg monocrotaline dissolved in 1% DMSO and then observed for the occurrence of PAH for up to four weeks, depending on the group. Control rats received 1% DMSO via intraperitoneal injection. Rats were injected with T16Ainh - A01 (0.33mg/kg) via the tail veins every other day for two weeks. After the experiments, the rats were anesthetized with 10% chloral hydrate and sacrificed. The heart tissues were quickly retrieved by opening the rats' chests for analysis. |
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Dosage form |
0.33mg/kg; every other day; 2 weeks; tail vein injection |
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Applications |
T16Ainh - A01 treatment alleviated the right ventricular hypertrophy in rats with PAH. |
| References: [1] Shi M, Wang J, Huang X, et al. Targeting TMEM16A/ANO1 inhibits the progression of BRAF mutant (V600E) melanoma through the MEK/ERK and AKT signaling pathways[J]. Genes & Diseases, 2024, 11(6): 101153. [2] Xie J, Liu W, Lv W, et al. Transmembrane protein 16A/anoctamin 1 inhibitor T16Ainh-A01 reversed monocrotaline-induced rat pulmonary arterial hypertension[J]. Pulmonary Circulation, 2020, 10(4): 2045894020946670. | |
| Cas No. | 552309-42-9 | SDF | |
| Chemical Name | 2-((5-ethyl-6-methyl-4-oxo-1,4-dihydropyrimidin-2-yl)thio)-N-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide | ||
| Canonical SMILES | O=C1N=C(NC(C)=C1CC)SCC(NC2=NC(C(C=C3)=CC=C3OC)=CS2)=O | ||
| Formula | C19H20N4O3S2 | M.Wt | 416.52 |
| Solubility | 5mg/ml in DMSO; 10mg/ml in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4008 mL | 12.0042 mL | 24.0085 mL |
| 5 mM | 480.2 μL | 2.4008 mL | 4.8017 mL |
| 10 mM | 240.1 μL | 1.2004 mL | 2.4008 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)