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Aquaporins Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Amyloid-β (2) Apoptosis (2) Aquaporin (10) Bacterial (2) Dihydroorotate Dehydrogenase (2) ERK (1) Ferroptosis (2) Fungal (1) Glutathione Peroxidase (2) Heme Oxygenase (HO) (2) Herbicide (1) Insecticide (2) Keap1-Nrf2 (2) Monoamine Oxidase (2) NF-κB (2) NOD-like Receptor (NLR) (1) p38 MAPK (1) PAI-1 (2) PI3K (2) PKC (2) Pregnane X Receptor (PXR) (2) PROTAC Linkers (2) Proton Pump (2) Pyroptosis (1) Reference Standards (2) Thrombin (2) Toll-like Receptor (TLR) (2) TRP Channel (2)
By Research Areas:	Cancer (6) Cardiovascular Disease (4) Infection (3) Inflammation/Immunology (7) Metabolic Disease (1) Neurological Disease (8)

By Targets:

Akt (2)

Amyloid-β (2)

Apoptosis (2)

Aquaporin (10)

Bacterial (2)

Dihydroorotate Dehydrogenase (2)

ERK (1)

Ferroptosis (2)

Fungal (1)

Glutathione Peroxidase (2)

Heme Oxygenase (HO) (2)

Herbicide (1)

Insecticide (2)

Keap1-Nrf2 (2)

Monoamine Oxidase (2)

NF-κB (2)

NOD-like Receptor (NLR) (1)

p38 MAPK (1)

PAI-1 (2)

PI3K (2)

PKC (2)

Pregnane X Receptor (PXR) (2)

PROTAC Linkers (2)

Proton Pump (2)

Pyroptosis (1)

Reference Standards (2)

Thrombin (2)

Toll-like Receptor (TLR) (2)

TRP Channel (2)

By Research Areas:

Cancer (6)

Cardiovascular Disease (4)

Infection (3)

Inflammation/Immunology (7)

Metabolic Disease (1)

Neurological Disease (8)

Inhibitors & Agonists

Inhibitory Antibodies

Natural
Products

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W008574

TGN-020 Maximum Cited Publications 21 Publications Verification	PROTAC Linkers	Inflammation/Immunology Cancer
TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC₅₀ of 3.1 μM . TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs .TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats .

HY-161834

RG100204 1 Publications Verification	Pyroptosis Aquaporin NOD-like Receptor (NLR) p38 MAPK	Infection Metabolic Disease Inflammation/Immunology
RG100204 is a selective, orally available inhibitor of the aquaporin AQP9. RG100204 directly inhibits AQP9 channel function, preventing the transmembrane transport of water, glycerol, and H ²O ². RG100204 reduces the activation of the NLRP3 inflammasome and p38 MAPK signaling pathways, thereby alleviating inflammation and pyroptosis. RG100204 reduces multi-organ dysfunction in a mouse sepsis model and shows glucose-regulating effects in diabetic db/db mice .

HY-W008574A

TGN-020 sodium Maximum Cited Publications 21 Publications Verification	PROTAC Linkers	Inflammation/Immunology Cancer
TGN-020 sodium is a selective Aquaporin 4 (AQP4) inhibitor with an IC₅₀ of 3.1 μM . TGN-020 sodium is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs . TGN-020 sodium alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats .

HY-126073

DFP00173 5+ Cited Publications	Aquaporin	Inflammation/Immunology Cancer
DFP00173 is a potent and selective aquaporin-3 (AQP3) inhibitor. DFP00173 inhibits mouse and human AQP3 with an IC₅₀ of ～0.1-0.4 μM. DFP00173 is selective for AQP3 over the homologous AQP isoforms AQP7 and AQP9 .

HY-126074

Z433927330 1 Publications Verification	Aquaporin	Others
Z433927330 is a potent and selective inhibitor of Aquaporin-7 (AQP7), less potently inhibits AQP3 and AQPs9, with IC₅₀s of ~0.2 µM, ~0.7 µM and ~1.1 µM for mAQP7, mAQP3 and mAQP9, respectively .

HY-N3097

Pellitorine	TRP Channel Amyloid-β Toll-like Receptor (TLR) Keap1-Nrf2 Heme Oxygenase (HO) Dihydroorotate Dehydrogenase Ferroptosis PAI-1 NF-κB ERK Proton Pump Glutathione Peroxidase Thrombin Insecticide Bacterial	Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria .

HY-115460

AER-271 1 Publications Verification	Aquaporin	Cardiovascular Disease Neurological Disease
AER-271, a phosphonate proagent derivative of AER-270, is an *aquaporin-4* (AQP4) inhibitor for the research of acute ischemic stroke .

HY-N4246

Bacopaside I	Aquaporin PKC Akt PI3K Apoptosis Monoamine Oxidase Pregnane X Receptor (PXR)	Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .

HY-N3097R

Pellitorine (Standard)	Reference Standards TRP Channel Amyloid-β Toll-like Receptor (TLR) Keap1-Nrf2 Heme Oxygenase (HO) Dihydroorotate Dehydrogenase Ferroptosis PAI-1 NF-κB Proton Pump Glutathione Peroxidase Thrombin Insecticide Bacterial	Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.

HY-N4246R

Bacopaside I (Standard)	Reference Standards PKC Akt PI3K Apoptosis Pregnane X Receptor (PXR) Monoamine Oxidase Aquaporin	Neurological Disease
Bacopaside I (Standard) is the analytical standard of Bacopaside I. This product is intended for research and analytical applications. Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .

HY-148823

RF03176	Aquaporin	Others
RF03176 is an aquaporin-9 (AQP-9) inhibitor, also exhibiting moderate inhibition effects on mAQP3 and mAQP7. RF03176 shows no activity against mAQP8 .

HY-18805

Nicotinanilide N-Phenylnicotinamide	Aquaporin	Neurological Disease
Nicotinanilide (N-Phenylnicotinamide) (Compound 12) is an aquaporin 4 (AQP4) inhibitor. Nicotinanilide can be used for research on diseases associated with AQP4 dysfunction, such as epilepsy and migraine .

HY-W017091

3-Phenoxy-1,2-propanediol	Aquaporin	Neurological Disease
3-Phenoxy-1,2-propanediol (compound 15) is a weak aquaporin 4 (AQP4) inhibitor . 3-Phenoxy-1,2-propanediol is an important intermediate for pharmaceuticals .

HY-P991869

Aquaporumab AQmabAM; rAb-53	Aquaporin	Neurological Disease
Aquaporumab (AQmabAM) is an engineered human monoclonal IgG antibody. Aquaporumab is a selective inhibitor of aquaporin 4 (AQP4), binding tightly to AQP4 and competitively displacing AQP4-IgG from serum [1][2]. Aquaporumab significantly reduces neuromyelitis optica lesions in spinal cord slice cultures and in mice receiving intracerebral injection of AQP4-IgG and complement [1][2]. Aquaporumab can be used for research on neuromyelitis optica spectrum disorders [1][2]."}

HY-N12990

Myrigalone A MyA	Herbicide Fungal	Others
Myrigalone A (MyA) is a plant ethylene biosynthesis inhibitor and natural herbicide . Myrigalone A possesses antioxidant, antifungal, and antimicrobial activities. Myrigalone A interferes with auxin homeostasis during seed germination. Myrigalone A delays seed germination, inhibits the formation of roots, hypocotyls, and root hairs, and causes developmental delay in specific organisms. Myrigalone A triggers the induction of detoxification programs, alters the metabolism of gibberellins, cis-(+)-12-oxophytodienoic acid, and jasmonic acid, disrupts the antioxidant system and oxidative signaling, and impairs the function of aquaporins and water uptake in imbibed seeds. Myrigalone A can be used in studies related to herbicides and plant growth regulators .

Cat. No.	Product Name	Target	Research Area	Image