Aquaporin

Atorvastatin Sodium (Lipitor) is a competitive inhibitor of HMG-CoA reductase and increases the expression of low density lipoprotein (LDL) receptors on hepatocytes. Atorvastatin Sodium treatment inhibits aquaporin 4 to reduce ischaemic brain oedema.

TGN-020 is an inhibitor of Aquaporin 4 (AQP4, IC50: 3.1 μM), the most abundant water channel in the brain.

DFP00173 is a potent and selective aquaporin 3 (AQP3) inhibitor, with an IC50 of approximately 0.1-0.4 μM for both mouse and human AQP3. It demonstrates selectivity for AQP3 compared to homologous AQP subtypes AQP7 and AQP9.

p-Tolylmaleimide (p Tolylmaleimide) is an inhibitor of the water channel and binds to Aquaporin Z.

TGN-073 is an enhancer of aquaporin 4 (AQP4), a water channel in astrocytes. It shows an increase in lymphatic transport in the rat brain by up to 41%.

TC-AQP1-1 is a blocker of the aquaporin 1 channel identified by virtual screening and inhibits water flux through hAQP1 in Xenopus laevis oocyte swelling assays at low micromolar concentrations.

AER-271 is an inhibitor of aquaporin-4.

AQP4 (205-215) is a fragment of the water channel protein Aquaporin-4 (AQP4). This protein is an autoimmune antigen in optic neuromyelitis and, upon binding with CD40, is upregulated and presented in B cells. AQP4 is associated with neuromyelitis optica (NMO), an autoimmune inflammatory disease of the central nervous system (CNS).

1. Steviol (NSC-226902), a natural sweetener, it inhibits proliferation of the gastrointestinal cancer cells intensively. 2. Steviol can induce a significant increase in CYP3A29 expression. 3. Steviol inhibits the proliferation of the human osteosarcoma U2OS cell line in a dose- and time-dependent manner. 4. Steviol can treat polycystic kidney disease, it slowed cyst growth, in part, by reducing AQP2 transcription, promoted proteasome, and lysosome-mediated AQP2 degradation.

AQP4 (201-220) TFA is an encephalitogenic epitope of AQP-4. This compound can induce experimental autoimmune encephalomyelitis (EAE), characterized by midline brain lesions, retinal abnormalities, and lesions at the grey/white matter boundary of the spinal cord. AQP-4 is the target antigen in neuromyelitis optica.

AQP4 (201-220) is the encephalitogenic epitope of AQP-4. AQP4 (201-220) can induce experimental autoimmune encephalomyelitis (EAE), characterized by midline brain lesions, retinal lesions, and lesions at the gray matter/white matter boundary of the spinal cord. AQP-4 is the target antigen in neuromyelitis optica.

AQP4 (205-215) TFA is a fragment of the water channel protein-4 (AQP4). AQP4 acts as an autoimmune antigen in neuromyelitis optica, upregulating and presenting in B cells upon binding with CD40. AQP4 is associated with neuromyelitis optica (NMO), an autoimmune inflammatory disease of the central nervous system (CNS).

Z433927330 is a potent and selective Aquaporin-7 (AQP7) inhibitor (IC50 of 0.2).

Bacopaside II is a potential anti-angiogenic agent, it can reduce endothelial cell migration and tubulogenesis and induce apoptosis.

ORI-TRN-002 is an AQP4 inhibitor with an IC50 value of 3 μM. It is applicable in the field of brain edema research.

Betamethasone acetate, the 21-acetate ester of betamethasone, is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.

1.Aristolactam I (Aristololactum) has cytotoxic potency, mediated through the induction of apoptosis in a caspase 3-dependent pathway. 2. The effects of Aristololactam I may be mediated by different mechanisms except TGF-beta1 pathway. 3. Aristololactam I may be one of toxic metabolites in Chinese herbs containing AA which participate in renal damage and fibrosis.

AQP3-IN-1 (compounds 3), an AQP3 inhibitor, exhibits an IC 50 of 8.91 μM and effectively inhibits melanoma cell proliferation [1].

RG100204 is an orally active AQP9 inhibitor with anti-inflammatory properties. It alleviates cardiac dysfunction (systolic and diastolic) induced by sepsis, improves renal dysfunction, and reduces the elevation of the cellular damage marker LDH.

Scaff10-8 is an inhibitor of AKAP-Lbc-RhoA interaction that acts by promoting the translocation of aquaporin-2 to the plasma membrane of renal collecting duct principal cells.

NMO-IgG blocker A-01 is a idiotype-specific blocker of neuromyelitis opticaimmunoglobulin g (nmo-igg) binding to aquaporin-4 (aqp4)

AqB011 is a selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration.

AqB007 is a selective blocker of the Aquaporin-1 ion channel conductance, thereby slowing cancer cell migration.

Dioleoylphosphatidylglycerol (DOPG), a naturally occurring phospholipid, is synthesized through the action of aquaporin 3 (AQP3) and phospholipase D2 (PLD2). It functions to suppress the production of inflammatory mediators by macrophages triggered by the activation of toll-like receptor 2 (TLR2) by heat shock protein B4 (HSPB4) [1].