Structure of T16Ainh-A01
CAS No.: 552309-42-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H315-H319 |
Precautionary Statements: | P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313-P362 |
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 |
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 |
Tags: T16Ainh-A01 | Chloride Channel | Cl− Channels | inhibitor | 552309-42-9 |
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