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Chemical Structure| 552309-42-9 Chemical Structure| 552309-42-9

Structure of T16Ainh-A01
CAS No.: 552309-42-9

Chemical Structure| 552309-42-9

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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).

Synonyms: T16A(inh)-A01

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Product Details of T16Ainh-A01

CAS No. :552309-42-9
Formula : C19H20N4O3S2
M.W : 416.52
SMILES Code : O=C(NC1=NC(C2=CC=C(OC)C=C2)=CS1)CSC3=NC(C)=C(CC)C(N3)=O
Synonyms :
T16A(inh)-A01
MDL No. :MFCD03278952
InChI Key :QSIYTNYMBWYHAA-UHFFFAOYSA-N
Pubchem ID :135460621

Safety of T16Ainh-A01

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313-P362

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse retinal rod bipolar cells 10 µM 200 milliseconds Inhibited outward rectifying current, confirming the voltage-dependent component of ANO1 Cells. 2020 Feb 26;9(3):543
SH-SY5Y cells 10–30 µM 24 hours Evaluate the effect of T16Ainh-A01 on HRSV-GFP expression, results showed significant reduction in HRSV-GFP expression Thorax. 2021 Jan;76(1):64-72
A549 cells 5–30 µM 24 hours Evaluate the effect of T16Ainh-A01 on HRSV-GFP expression, results showed significant reduction in HRSV-GFP expression Thorax. 2021 Jan;76(1):64-72
HaCaT keratinocytes 30 µM 3 days Inhibition of HaCaT cell proliferation and reduction of pERK1/2 phosphorylation Int J Mol Sci. 2021 Jul 1;22(13):7145
Vascular smooth muscle cells (VSMCs) 10 µM 30 minutes Inhibiting TMEM16A activity, significantly reducing the expression of VCAM-1 and ICAM-1 Biomedicines. 2022 Oct 31;10(11):2760
Mouse retinal rod bipolar cells 40 µM 300 seconds Inhibited ANO1 tail current (I tail), indicating ANO1 is activated by Ca2+ Cells. 2020 Feb 26;9(3):543
Mouse cardiac vascular endothelial cells (CVECs) 30 µM 48 hours To evaluate the effect of T16Ainh-A01 on CVECs proliferation, results showed T16Ainh-A01 did not affect cell growth Br J Pharmacol. 2014 Aug;171(15):3680-92
Dorsal root ganglia neurons 20 µM and 100 µM 90 seconds ANO1 blockade with T16Ainh-A01 significantly inhibited the PGE2-evoked axonal depolarisation Sci Rep. 2024 Jul 29;14(1):17360

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6N mice Cerulein-induced acute pancreatitis model Intraperitoneal injection 1 mg/kg Single injection, lasting 12 hours To investigate the effect of T16Ainh-A01 on the acute pancreatitis mouse model, results showed that T16Ainh-A01 ameliorated pancreatic damage and reduced IL-6 levels in serum and pancreatic tissues. J Adv Res. 2020 Jan 21;23:25-35
Genetically epilepsy-prone rats (GEPR-3s) Genetically epilepsy-prone rat model Oral 10 mg/kg Single dose, tested 30 minutes after administration To evaluate the effects of T16Ainh-A01 on acoustically evoked seizures in GEPR-3s. Results showed that T16Ainh-A01 pretreatment did not significantly alter the incidence of WRSs and GTCSs, seizure latency, seizure duration, or seizure severity. Biomedicines. 2022 Feb 15;10(2):449
Sprague-Dawley rats Chronic constriction injury (CCI) model Intrathecal injection 10 μg Once every 6 hours, totally five times To evaluate the effect of T16Ainh-A01 on CCI-induced neuropathic pain. Results showed that T16Ainh-A01 significantly alleviated thermal hyperalgesia, reduced the excitability of DRG neurons, and decreased TMEM16A expression. Neural Regen Res. 2019 Jun;14(6):1091-1098
Guinea pig Tracheal rings Organ baths 10 μM, 50 μM, 100 μM 30-minute intervals To investigate the relaxant effect of T16Ainh-A01 on acetylcholine-induced contraction. Results showed that 50 μM and 100 μM T16Ainh-A01 significantly relaxed the acetylcholine-induced contraction. Anesthesiology. 2015 Sep;123(3):569-81
BALB/c mice IMQ-induced psoriasis-like skin injury model Topical application on ears 30 µM and 100 µM Once daily for 7 consecutive days Alleviation of psoriasis-like symptoms and reduction of ANO1 and pERK1/2 expression Int J Mol Sci. 2021 Jul 1;22(13):7145
Mice Pain-related behavior model Hind paw injection 300 μM Single injection, observed for 5 minutes Investigate the effect of ANO1 antagonist T16Ainh-A01 on capsaicin-induced pain-related behaviors, finding that A01 significantly reduced capsaicin-induced pain behaviors Proc Natl Acad Sci U S A. 2015 Apr 21;112(16):5213-8

Protocol

Bio Calculators
Preparing Stock Solutions 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

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