trabecular

CK-666 is a cell-permeable inhibitor of the actin-related protein Arp2 3 complex, binding to and stabilizing its inactive state, thereby preventing the movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) configuration.

1. Poncirin (Isosakuranetin-7-neohesperidoside) shows a significant in vitro inhibitory effect on the growth of the human gastric cancer cells, SGC-791, in a dose-dependent manner. 2. Poncirin prevents adipogenesis, enhances osteoblast differentiation in mesenchymal stem cellsincreased bone mineral density, and improves trabecular microarchitecture likely reflect increases bone formation and decreases bone resorption in GIO mice.

Tetrahydrocortisol (Tetrahydrohydrocortisone) is a metabolite of neurosteroids and cortisol, a GABAA receptor antagonist, and also capable of lowering intraocular pressure.

Sphinganine-1-phosphate (d17:0) is a sphingolipid analog of sphinganine-1-phosphate (d18:0) and sphingosine-1-phosphate (d18:1) that has a 17-carbon base. Sphinganine-1-phosphate (d17:0) levels are lower in surgical and cadaver trabecular meshwork samples isolated from patients with primary open angle glaucoma compared with control samples.

C16 Sphingosine-1-phosphate (C16 S1P) is a derivative of sphingosine-1-phosphate that binds to S1P1/EDG-1, S1P3/EDG-3, and S1P2/EDG-5 receptors with affinities of 115%, 83%, and 103%, respectively, relative to S1P in CHO cells. C16 S1P was increased in postmortem primary open angle glaucoma trabecular meshwork samples.

Verosudil (AR-12286) is a highly potent Rho kinase (ROCK) inhibitor with a Ki of 2 nM and 2 nM against ROCK1 and ROCK2, respectively. AR-12286 mitigates steroid-induced intraocular pressure in mice by decreasing intraocular pressure through enhanced outflow of aqueous humor via the trabecular meshwork.

ROCK-IN-4 is a potent ROCK inhibitor that maintains NO release capacity, reversibly depolymerizes F-actin, and blocks mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be utilized to study glaucoma or high intraocular pressure.

KR-67607, also known as NTX-101 is novel selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. KR-67607 decreased 4-hydroxynonenal expression and increased antioxidant and mucus secretion in BAC-treated rat eyes. KR-67607 showed its protective effects against ischemia-reperfusion-induced eye injury. KR-67607 effectively reduced cortisol levels in mouse eyes and maintained the trabecular meshwork (TM) structure in the presence of transient ischemic stress. Furthermore, KR-67607 reversed the elevation of intra-ocular pressure (IOP), suggesting that the TM structure maintained by KR-67607 prevented the excessive rise in IOP that exacerbates glaucoma.

2MD, an orally active vitamin D analog, both stimulates periosteal bone formation and decreases trabecular bone resorption, effectively restoring trabecular and cortical bone mass and strength. Additionally, 2MD regulates genes related to intraocular pressure (IOP) and reduces IOP in non-human primates [1] [2].

VnP-16, a synthetic peptide fragment mirroring amino acids 270-281 of vitronectin (a multifunctional glycoprotein involved in cell attachment, migration, and spreading), promotes attachment and spreading of isolated human osteogenic cells. This effect is reversible with β1 integrin siRNA knockdown when VnP-16 is applied at 9.1 µg/cm2 on cell plates. The compound enhances osteogenesis in human skin-derived mesenchymal precursors and MC3T3-E1 mouse calvarial osteoblast precursors. Furthermore, in vivo studies show VnP-16 mitigates IL-1α-induced bone loss, reduces calvarial osteoclast numbers in mice, increases bone mineral density, and lessens trabecular bone loss in a mouse model of ovariectomy-induced bone loss.