S1351 |
Ivermectin
|
Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
-
Viruses, 2025, 17(2)220
-
J Clin Invest, 2024, 134(22)e181314
-
Viruses, 2024, 16(4)640
|
|
S1698 |
Torsemide
|
Torsemide (AC-4464, JDL-464) is a pyridyl sulfonylurea with a chemical structure between that of traditional loop diuretics and Cl- channel blockers, used to treat hypertension. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cell Chem Biol, 2021, S2451-9456(21)00442-6
|
|
S0454 |
Adjudin
|
Adjudin (AF-2364), a potent male contraceptive, is a potent blocker of Cl⁻ channels. Adjudin exhibits anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation. |
-
Brain Res Bull, 2022, 182:80-89
|
|
S1675 |
Lubiprostone
|
Lubiprostone (RU 0211,SPI-0211) is an activator of ClC-2 chloride channels, used in the management of idiopathic chronic constipation. |
|
|
F1383 |
Phospho-IP3 Receptor (Ser1756) Rabbit mAb
|
|
|
|
E4665New |
NMD670
|
NMD670 is a first-in-class small molecule inhibitor of skeletal muscle-specific chloride channel (ClC-1) with an EC50 of 1.6 μM. It improves muscle weakness and fatigue in neuromuscular diseases and may serve as a potential therapeutic approach for Myasthenia Gravis (MG). |
|
|
S8279 |
(±)-Shikonin
|
(±)-Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
-
Elife, 2024, 12RP91141
-
Elife, 2024, 12RP91141
-
Mol Ther Methods Clin Dev, 2024, 32(3):101307
|
|
E7830New |
R(+)-Methylindazone
|
R(+)-Methylindazone (R(+)-IAA-94) is a potentand specific indanyloxyacetic inhibitor of the renal epithelial chloride channel and exacerbates myocardial infarction by impairing mitochondrial calcium retention capacity (CRC), leading to mitochondrial permeability transition pore (mPTP) opening and increased cell death during ischemia-reperfusion injury. |
|
|
S3264 |
Atractyloside potassium salt
|
Atractyloside potassium salt (ATR potassium salt), a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum (Cang'erzi), is a powerful and specific inhibitor of mitochondrial ADP/ATP carriers. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. |
|
|
S0125 |
CaCCinh-A01
|
CaCCinh-A01 (TMEM16 Blocker I) is a blocker of TMEM16A with IC50 of 2.1 μM. CaCCinh-A01 is also an inhibitor of calcium-activated chloride channel (CaCC) with IC50 of ~ 10 μM. |
|
|
A2726 |
Anti-ANO1 / TMEM16A
|
Anti-ANO1 / TMEM16A is a humanized monoclonal antibody that binds to human TMEM16A and modulates its activity, with potential anti-tumor activity. MW: 146.8 KD. |
|
|
S4339 |
Meticrane
|
Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension. |
|
|
S3807 |
Dehydroandrographolide
|
Dehydroandrographolide, isolated from Andrographis paniculata (Burm. F.) Nees (Chuan-xin-lian), is a novel TMEM16A inhibitor and possesses multiple pharmacological activities, including anti-inflammation, anti-cancer, anti-bacterial, anti-virus and anti-hepatitis activity. |
|
|
S6439 |
Talniflumate
|
Talniflumate (MSI-1995) is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma. Talniflumate is also an inhibitor of human calcium-activated chloride channels. |
-
Toxicol Lett, 2025, 406:31-37
-
Acta Pharm Sin B, 2023, 13(2):662-677
|
|
S2955 |
NS1652
|
NS1652 is a reversible chloride channel blocker, potently inhibits the chloride conductance (IC50 = 1.6 μM) in human and mouse red blood cells, but only weakly volume activated anion conductance (VRAC) (IC50 = 125 μM) in HEK293 cells. |
|
|
S6470 |
Fluralaner
|
Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls) |
|
|
S1203 |
T16Ainh-A01
|
T16Ainh-A01 is a potent and selective inhibitor of calcium-activated chloride channel (CaCC)/transmembrane protein 16A (TMEM16A, ANO1) with IC50 of 1.8 μM.
|
|
|
S1698 |
Torsemide
|
Torsemide (AC-4464, JDL-464) is a pyridyl sulfonylurea with a chemical structure between that of traditional loop diuretics and Cl- channel blockers, used to treat hypertension. |
- J Immunother Cancer, 2024, 12(11)e009805
- Cell Chem Biol, 2021, S2451-9456(21)00442-6
|
|
S0454 |
Adjudin
|
Adjudin (AF-2364), a potent male contraceptive, is a potent blocker of Cl⁻ channels. Adjudin exhibits anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation. |
- Brain Res Bull, 2022, 182:80-89
|
|
E4665New |
NMD670
|
NMD670 is a first-in-class small molecule inhibitor of skeletal muscle-specific chloride channel (ClC-1) with an EC50 of 1.6 μM. It improves muscle weakness and fatigue in neuromuscular diseases and may serve as a potential therapeutic approach for Myasthenia Gravis (MG). |
|
|
S8279 |
(±)-Shikonin
|
(±)-Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition. |
- Elife, 2024, 12RP91141
- Elife, 2024, 12RP91141
- Mol Ther Methods Clin Dev, 2024, 32(3):101307
|
|
E7830New |
R(+)-Methylindazone
|
R(+)-Methylindazone (R(+)-IAA-94) is a potentand specific indanyloxyacetic inhibitor of the renal epithelial chloride channel and exacerbates myocardial infarction by impairing mitochondrial calcium retention capacity (CRC), leading to mitochondrial permeability transition pore (mPTP) opening and increased cell death during ischemia-reperfusion injury. |
|
|
S3264 |
Atractyloside potassium salt
|
Atractyloside potassium salt (ATR potassium salt), a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum (Cang'erzi), is a powerful and specific inhibitor of mitochondrial ADP/ATP carriers. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. |
|
|
S0125 |
CaCCinh-A01
|
CaCCinh-A01 (TMEM16 Blocker I) is a blocker of TMEM16A with IC50 of 2.1 μM. CaCCinh-A01 is also an inhibitor of calcium-activated chloride channel (CaCC) with IC50 of ~ 10 μM. |
|
|
S4339 |
Meticrane
|
Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension. |
|
|
S3807 |
Dehydroandrographolide
|
Dehydroandrographolide, isolated from Andrographis paniculata (Burm. F.) Nees (Chuan-xin-lian), is a novel TMEM16A inhibitor and possesses multiple pharmacological activities, including anti-inflammation, anti-cancer, anti-bacterial, anti-virus and anti-hepatitis activity. |
|
|
S6439 |
Talniflumate
|
Talniflumate (MSI-1995) is an anti-inflammatory molecule studied and used as a mucin regulator in the treatment of cystic fibrosis, chronic obstructive pulmonary disease (COPD) and asthma. Talniflumate is also an inhibitor of human calcium-activated chloride channels. |
- Toxicol Lett, 2025, 406:31-37
- Acta Pharm Sin B, 2023, 13(2):662-677
|
|
S2955 |
NS1652
|
NS1652 is a reversible chloride channel blocker, potently inhibits the chloride conductance (IC50 = 1.6 μM) in human and mouse red blood cells, but only weakly volume activated anion conductance (VRAC) (IC50 = 125 μM) in HEK293 cells. |
|
|
S6470 |
Fluralaner
|
Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls) |
|
|
S1203 |
T16Ainh-A01
|
T16Ainh-A01 is a potent and selective inhibitor of calcium-activated chloride channel (CaCC)/transmembrane protein 16A (TMEM16A, ANO1) with IC50 of 1.8 μM.
|
|
|