Glaucoma

Echothiopate iodide (Echothiophate iodide) is an acetylcholinesterase (AChE) inhibitor. Echothiopate iodide irreversibly inhibits acetylcholinesterase, prevents the enzymatic hydrolysis of acetylcholine, and increases the local acetylcholine concentration in the ciliary muscle, thereby driving muscarinic receptor downregulation and regulatory hyposensitivity to Pilocarpine Hydrochloride. Echothiopate iodide can be used in the study of glaucoma.

Echothiopate chloride (Echothiophate chloride) is an acetylcholinesterase (AChE) inhibitor. Echothiopate chloride irreversibly inhibits acetylcholinesterase, prevents the enzymatic hydrolysis of acetylcholine, and increases the local acetylcholine concentration in the ciliary muscle, thereby driving muscarinic receptor downregulation and regulatory hyposensitivity to Pilocarpine Hydrochloride. Echothiopate chloride can be used in the study of glaucoma.

ROCK2-IN-20 is a selective ROCK2 inhibitor with an IC₅₀ value of 12 nM. ROCK2-IN-20 can be used for research on multiple sclerosis, pulmonary arterial hypertension, and glaucoma.

Besvoprost is a prostaglandin receptor activator with antiglaucoma activity. Besvoprost can be used for the research of glaucoma.

TAT-N24 is a cell-penetrating peptide and also an inhibitor of p55PIK. TAT-N24 disrupts the interactions between p55PIK and p53, PCNA or Rb, blocks the p53-dependent ubiquitin-mediated degradation process, and inhibits the nuclear translocation and phosphorylation of NF-κB p65. TAT-N24 enhances MMS-induced p53-dependent cell apoptosis, inhibits DNA synthesis, reduces the expression of Cyclin D1, and induces cell cycle arrest at the G0/G1 or S phase. TAT-N24 inhibits the activation of NLRP3 and NLRC4 inflammasomes, reduces the expression of ZBP1-PANoptosome components, and suppresses PANoptosis. TAT-N24 can be used in research related to leukemia, colon cancer, cervical cancer, liver cancer, corneal neovascularization, restenosis and acute glaucoma.

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.

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.

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.

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.

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.

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.

NCX-278 is a human carbonic anhydrase inhibitor with a 13 nM K_i for hCA II, 410 nM K_i for hCA I, 181 nM K_i for hCA IV, and selective inhibition of hCA II over hCA IV. NCX-278 is a potent and effective stimulator of NO/sGC/cGMP signaling with an EC₅₀ of 2.05 lM. NCX-278 exerts NO-mediated vascular relaxant effects. NCX-278 lowers intraocular pressure in normotensive rabbits. NCX-278 can be used for the research of open-angle glaucoma.

AL-38022A is a potent and selective 5-HT₂ receptor agonist (K_i ≤2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. AL-38022A potently stimulates functional responses via 5-HT₂ receptor subtypes including [Ca²⁺]_i mobilization and tissue contractions with apparently similar potencies and intrinsic activities. AL-38022A fully generalizes to the (±)-1-(2,5-dimethoxy 4-methylphenyl)-2-aminopropane hydrochloride (DOM) stimulus in drug discrimination paradigms. AL-38022A can be used for the glaucoma research.