Visual System Disease

RX-021 is a ROCK1 and ROCK2 inhibitor with IC₅₀ values of 30.01 nM and 34.31 nM, respectively. RX-021 induces reversible morphological changes in human trabecular meshwork cells, maintains the survival of retinal ganglion cells, restores electroretinogram responses, and improves retinal histopathological changes. RX-021 achieves sustained reduction of intraocular pressure in a mouse model of ocular hypertension. RX-021 can be used for the research of glaucoma.

RX-044 is a ROCK1/ROCK2 inhibitor with ROCK1 IC₅₀ 10.01 nM and ROCK2 IC₅₀ 9.68 nM, and demonstrates kinase selectivity. RX-044 induces reversible cell retraction, modulates cytoskeletal organization via F-actin depolymerization, inhibits cell contractility, and attenuates TGF-β2-induced cell migration. RX-044 preserves retinal ganglion cell survival, restores electroretinography responses, and ameliorates histopathological changes. RX-044 lowers intraocular pressure in a mouse ocular hypertension model. RX-044 shows no cytotoxicity in target cells. RX-044 exhibits initial ocular irritation that subsides with extended dosing. RX-044 can be used for the research of glaucoma.

Nocarnickelamide B TFA is a ROCK1/2 inhibitor with IC₅₀ values of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B TFA inhibits the activation of ROCK-regulated cytoskeletal contraction markers (especially myosin light chain) in human trabecular meshwork cells. Nocarnickelamide B TFA can be used in the research of glaucoma.

MTS peptide is a short peptide with a mitochondria-targeting sequence. In F-M-LNP, MTS peptide is displayed on the particle surface via thiol-maleimide conjugation, and is specifically responsible for being recognized by the mitochondrial proteins TOMM20/22, "anchoring" the nanoparticles to the outer mitochondrial membrane, followed by membrane potential-independent bilayer membrane penetration mediated by fluorinated lipids. MTS peptide can be used in the research of Leber's hereditary optic neuropathy.

COX-2/CA II-2 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-2 inhibits COX-2 with an IC₅₀ value of 0.05 μM (SI = 12.02 vs COX-1) and hCA II with a K_i value of 62.6 nM (SI = 704.2 vs hCA I). COX-2/CA II-2 demonstrates significant analgesic and anti-inflammatory effects with rapid onset and sustained duration in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits a gradual intraocular pressure (IOP)-lowering effect without statistical significance relative to the sham-treated eye in rabbit glaucoma models. COX-2/CA II-2 can be used for anti-inflammatory, analgesic and antiglaucoma research.

COX-2/CA II-1 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-1 inhibits COX-2 with an IC₅₀ value of 0.13 μM (SI = 9.25 vs COX-1) and hCA II with a K_i value of 39.1 nM (SI = 933.8 vs hCA I). COX-2/CA II-1 demonstrates significant analgesic and anti-inflammatory effects in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits intraocular pressure (IOP)-lowering effects in rabbit glaucoma models. COX-2/CA II-1 can be used for anti-inflammatory, analgesic and antiglaucoma research.

VEGFR/PDGFR/CA II-IN-1 is a VEGFR/PDGFR/CA II inhibitor. VEGFR/PDGFR/CA II-IN-1 potently inhibits VEGFR2 (IC₅₀ = 62.66 nM), PDGFRα (IC₅₀ = 18.65 nM), PDGFRβ (IC₅₀ = 5.23 nM), and hCA II (K_i = 19.4 nM), with weaker activity against hCA I (K_i = 154.2 nM) and hCA IX (K_i = 121.0 nM). VEGFR/PDGFR/CA II-IN-1 exhibits potent antiproliferative activity in VEGFR2-BAF3 cells and robust inhibition of angiogenesis in human umbilical vein endothelial cells (HUVECs). VEGFR/PDGFR/CA II-IN-1 inhibits the formation of corneal neovascularization in rabbits through multiple signaling pathways, and significantly reduced intraocular pressure (IOP) in both acute and chronic glaucoma models. VEGFR/PDGFR/CA II-IN-1 can be used to study neovascular glaucoma (NVG).

CAII-IN-16 is a selective inhibitor of carbonic anhydrase II (CA II), with an IC₅₀ of 0.5 nM against hCA II. CAII-IN-16 exhibits excellent intraocular pressure-lowering activity in a rabbit glaucoma animal model. CAII-IN-16 can be used for the research of glaucoma.

MRS2768 is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y₂-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.

N-Acetyl-L-leucyl-L-leucyl-L-methional is a Calpain II inhibitor with an IC₅₀ of 0.24 μM against porcine Calpain II. N-Acetyl-L-leucyl-L-leucyl-L-methional forms a stable tetrahedral adduct with the thiol group at the active site of Calpain II, thereby inhibiting proteolytic activity. N-Acetyl-L-leucyl-L-leucyl-L-methionally inhibits cathepsins in a non-selective manner. N-Acetyl-L-leucyl-L-leucyl-L-methional reduces SARS-CoV-2 infection levels in human coronary artery endothelial cells in vitro. N-Acetyl-L-leucyl-L-leucyl-L-methional can be used in research related to cataracts and coronavirus infections.

A3AR antagonist-8 is a selective A3 adenosine receptor antagonist with a K_i of 98 nM for human A3 adenosine receptor. A3AR antagonist-8 can be used for the research of glaucoma, chronic renal disease, acute renal ischemia and reperfusion injury, and cancer.

EYE1090 is an orally active VEGFR2 inhibitor with an IC₅₀ of 3 nM. EYE1090 inhibits angiogenesis, endothelial migration, VEGFR2-induced retinal leakage, and reduces choroidal neovascularization lesion size in mice. EYE1090 can be used for the research of age-related macular degeneration, diabetic retinopathy, choroidal neovascularization.

NG004 is a fully human monoclonal antibody targeting Nogo-A. NG004 reduces retinal Nogo-A levels, blocks the binding of the Nogo-A-receptor complex, and neutralizes the Nogo-A protein. NG004 can be used in studies related to diabetic retinopathy, stroke and acute spinal cord injury.

PF-04475270 is a prodrug of CP-734432 (HY-119236), as well as an agonist of the EP4 prostaglandin receptor, with IC₅₀ values of 2 nM and 8 nM against human and canine sources, respectively. PF-04475270 is rapidly hydrolyzed into its active metabolite CP-734432 by ocular esterases or corneal homogenate, stimulates cAMP production, and activates cAMP response element-mediated β-lactamase activity in cells expressing EP4. PF-04475270 can be used in research related to glaucoma.

Ferroptosis-IN-25, Trolox (HY-101445) derivative, is a selective ferroptosis inhibitor. Ferroptosis-IN-25 selectively inhibits ferroptosis by scavenging ROS and suppressing lipid peroxidation independently of glutathion. Ferroptosis-IN-25 reduces corneal neovascularization and edema in murine corneal alkali burn models via topical administration.Ferroptosis-IN-25 can be used for the research of ocular surface diseases.

CAII-IN-15 is a potent carbonic anhydrase II (CA II) inhibitor with a hCA II IC₅₀ of 10 nM. CAII-IN-15 elevates cGMP levels, releases nitric oxide, reduces oxidative stress, and exhibits neuroprotective activity in vitro. CAII-IN-15 inhibits NLRP3 inflammasome activation, reduces neuronal apoptosis. CAII-IN-15 reduces Intraocular pressure (IOP) in rabbits. CAII-IN-15 can be used for the research of glaucoma.

Neuro-DiO 4-chlorobenzenesulfonate is a hydrophobic C₁₈ alkyl chain carbocyanine dye with green fluorescence, commonly used as a vascular marker, cell internalizer and deposition agent. Neuro-DiO 4-chlorobenzenesulfonate inserts its alkyl chain into the endothelial plasma membrane via liposome-mediated perfusion to achieve vascular labeling. Neuro-DiO chlorobenzenesulfonate can also stain the cell membrane and cytoplasm of cancer cells to assist in confocal microscopy observations. Neuro-DiO chlorobenzenesulfonate can be released from nanosponges and accumulate on the surface of mouse retina, then internalize into retinal ganglion cells, which is applicable to researches related to glaucoma and other diseases. It should be noted that during liposome-mediated vascular staining in mice, Neuro-DiO 4-chlorobenzenesulfonate may cause leakage of airway lavage fluid.

Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [³H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia.

ICI 147798 is an orally effective β-adrenoceptor antagonist with a pK_B of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β₁-adrenoceptors, and shows surmountable competitive antagonism against β₂-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure.

AL-6556 is a full agonist of the DP receptor and a partial agonist of the EP2 receptor. AL-6556 has an EC₅₀ of 799 nM for bovine DP, a K_i of 3200 nM for human DP, and an EC₅₀ of 1180 nM for human EP2, with selectivity over EP3, FP, IP, TP and 19 non-prostaglandin receptors. AL-6556 stimulates cAMP production via receptor activation and reduces intraocular pressure through aqueous humor inflow and outflow mechanisms. AL-6556 can be used in research related to ocular hypertension and glaucoma.