Glaucoma

CAI/II-IN-12 is a potent and hCAI (IC₅₀ = 7.12 μM, K_i = 9.26 μM) and hCAII (IC₅₀ = 10.62 μM, K_i = 11.72 μM) dual inhibitor. CAI/II-IN-12 has a strong affinity for the active sites of CYP17A1, hCAI, and hCAII enzymes. Compound CAI/II-IN-12 exhibits rapid conformational stabilization, particularly in the CYP17A1 complex. CAI/II-IN-12 can be used for the study of prostate cancer therapy and glaucoma.

(Rac)-Sezolamide hydrochloride (MK-927; (Rac)-MK 417) is a carbonic anhydrase inhibitor (CAI) (K_i: 12.0 nM). (Rac)-Sezolamide hydrochloride has a topical intraocular pressure (IOP) lowering effect. (Rac)-Sezolamide hydrochloride can be used in glaucoma research.

2-MeSADP is a P2Y receptor agonist, with an EC₅₀ of 5 nM for human P2Y12, EC₅₀ values of 19 nM and 13 nM for human P2Y13, and an EC₅₀ of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma.

Brovincamine is an orally active slow Ca²⁺ channel blocker and vasodilator. Brovincamine reduces Ca²⁺ influx across the plasma membrane by blocking Ca²⁺ channels. Brovincamine inhibits catecholamine secretion, cholinergic function, autonomic parasympathetic nervous system activity, cerebrovascular resistance, and nerve stimulation-induced convulsive responses. Brovincamine induces cerebrovascular, coronary, and intracranial vasodilation, improves cerebral cortical microcirculation, enhances cerebral metabolic activity, and increases capillary clearance efficiency. Brovincamine can be used in research related to cerebral ischemic diseases, cardiac ischemic diseases, and normal-tension glaucoma.

Tazbentetol (Phenylbenzothiazole-PEG4-OH) is a synaptogenic compound. Tazbentetol partially preserves inner retinal neurotransmission function and maintains retinal function. Tazbentetol increases dendritic spine glutamatergic synapses via cytoskeleton signaling pathways, enhances synaptic density both in vitro and in vivo, and restores glutamatergic synapses. Tazbentetol improves the progression of motor symptoms and enhances memory. Tazbentetol can be used in the research of glaucoma, diabetic retinopathy and amyotrophic lateral sclerosis.

CP 132484 is a rat 5-HT_2A receptor agonist with a K_i of 1.1 nM and an IC₅₀ of 2.8 nM, and it exhibits over 40-fold selectivity over rat 5-HT1A receptors and bovine 5-HT1D receptors. CP 132484 stimulates phosphoinositide hydrolysis and intracellular calcium mobilization. CP 132484 can be used for research into diseases such as glaucoma.

Deacetyltrimepranol (Deacetylmetipranolol) is the active metabolite of metipranolol (HY-121567), a β-adrenergic receptor blocker. Deacetyltrimepranol can be used in the research of hypertension.

Cotosudil hydrochloride is a ROCK kinase inhibitor that can be used in studies on glaucoma or ocular hypertension.

ROCK-IN-13 is a ROCK2 inhibitor with an IC₅₀ of 8 nM against human ROCK2. ROCK-IN-13 has the potential for use in the research of diseases such as multiple sclerosis, glaucoma, and cardiovascular diseases.

CK-102 is an interleukin-1 (IL-1) inhibitor. CK-102 reduces mRNA synthesis. CK-102 does not inhibit DNA synthesis. CK-102 only slightly inhibits protein synthesis, or has no effect on it. CK-102 delays wound healing after ophthalmic surgery and prolongs the failure time of trabeculectomy fistulas. CK-102 inhibits lens protein-induced ocular inflammation at both early and late stages. CK-102 inhibits endotoxin-induced uveitis. CK-102 does not inhibit interleukin-1-induced uveitis. CK-102 can be used in research related to glaucoma filtration failure and uveitis.

KR-67607 is a selective 11β-HSD1 inhibitor, with an IC₅₀ value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease.

S58 aptamer is a ssDNA aptamer targeting transforming growth factor-beta receptor II (TGF-β RII). S58 aptamer inhibits the TGF-β RII interaction with TGF-β. S58 aptamer effectively improves glaucoma filtration surgery (GFS) surgical outcomes by activating the intracellular antioxidant defense PI3K/Akt/Nrf2 signaling pathway.

mNOX-E36 is a murine-specific analogue of NOX-E36 (HY-148100), an anti-CCL-2 L-RNA aptamer that binds and neutralises the mouse chemokine CCL-2. mNOX-E36 reduces scarring in an experimental murine model of glaucoma filtration surgery (GFS). mNOX-E36 ameliorates lupus nephritis in mice. mNOX-E36 can be used for GFS and lupus nephritis research.

ML-7 is a selective and highly specific myosin light chain kinase (MLCK) inhibitor that acts as a trabecular meshwork (TM) relaxant. ML-7 enhances Quinocetone (HY-123581)-induced phosphorylation of ERK, p38 MAPK and JNK, attenuates Akt activation, and promotes apoptosis of hepatocellular carcinoma cells. ML-7 reduces Th2 cytokine secretion by inhibiting MLCK, while alleviating smooth muscle hyperplasia and collagen deposition. As a non-antibiotic adjuvant, ML-7 restores the sensitivity of drug-resistant bacteria to Tigecycline (HY-B0117). ML-7 can be used in research related to glaucoma, hepatocellular carcinoma, asthma, and Klebsiella pneumoniae infection.