Retinopathy

Aminoguanidine (Pimagedine) hydrochloride is an inhibitor of diamine oxidase (DAO) and nitric oxide synthase (NOS). Aminoguanidine hydrochloride can reduce the formation of advanced glycation end products (AGEs). Aminoguanidine hydrochloride has a dose-dependent inhibitory effect on Doxorubicin (HY-15142)-induced cell apoptosis. Aminoguanidine hydrochloride has antioxidant properties. Aminoguanidine hydrochloride can be used in the research of diabetic nephropathy.

HTRA1-IN-1 is a potent and selective high temperature requirement A serine peptid 1 (HTRA1) inhibitor with an IC₅₀ of 13 nM. HTRA1-IN-1 can be used for the research of HTRA1-related diseases, such as age-related macular degeneration (AMD), osteoarthritis, and rheumatoid arthritis.

Cenupatide (UPARANT) is a uPAR and FPR antagonist with anti-angiogenic, anti-inflammatory, and vascular barrier regulatory activities, as well as high stability and resistance to enzymatic degradation in blood/plasma. Cenupatide blocks the uPAR-FPR interaction, reduces VEGF-induced phosphorylation levels of AKT, VEGFR-2, STAT3, JNK, p38 MAPK, ERK1/2, and NF-κB p65, and inhibits αvβ3 integrin activation. Cenupatide suppresses endothelial cell migration, invasion, tube formation, and angiogenic signaling pathways, restores tight junctions and blood-retinal barrier integrity, reduces pro-inflammatory marker levels, and inhibits apoptosis. Cenupatide reduces retinal neovascularization, renal fibrosis, and vascular leakage, and restores visual function in preclinical models. Cenupatide is applicable to research related to retinopathy, diabetic complications, ocular diseases, cancer, and inflammatory diseases.

JB-1, an IGF-I analog, is a selective IGF-I receptor inhibitor that does not interact with IGF-II. JB-1 competes with IGF-I for binding to IGF-1R and blocks receptor autophosphorylation. JB-1 increases the level of sVEGFR-1. JB-1 normalizes retinal abnormalities, including reducing retinal neovascularization. JB-1 is applicable to studies related to oxygen-induced retinopathy.

TREM-1 inhibitory peptide GF9 (Human TREM-1 (213-221)) is a TREM-1 inhibitor. TREM-1 inhibitory peptide GF9 blocks the TREM-1 signaling pathway via a ligand-independent mechanism, spontaneously inserts into the cell membrane to dissociate TREM-1 from DAP-12, and functions through the Signaling Chain Homooligomerization (SCHOOL) model. TREM-1 inhibitory peptide GF9 reduces the levels of TNFα, IL-1β, IL-6, and M-CSF. TREM-1 inhibitory peptide GF9 inhibits tumor growth, prolongs the survival of mice with pancreatic cancer models, ameliorates collagen-induced arthritis, and exerts protective effects on bone and cartilage simultaneously. TREM-1 inhibitory peptide GF9 can be used in research related to arthritis, pancreatic cancer, retinopathy, alcoholic liver disease, and liver cancer.

EYE1118 is an orally active, photoactivatable VEGFR2 inhibitor without acute hepatotoxicity. EYE1118 mediates light-enhanced inhibition via azide-functionalized receptor binding, and can utilize light-guided targeting to regulate its biodistribution in vivo. EYE1118 effectively inhibits angiogenesis, endothelial cell migration, VEGF-induced retinal leakage, and the size of choroidal neovascular lesions. EYE1118 has been applied in studies related to age-related macular degeneration, diabetic retinopathy, and choroidal neovascularization.

SU10944 is a selective, orally active VEGFR inhibitor, with an IC₅₀ of 6 nM against VEGFR-1, an IC₅₀ of 96 nM and a K_i of 21 nM against VEGFR-2. SU10944 only exhibits weak inhibitory activity against PDGFRβ (IC₅₀ = 1 μM), SCFR (IC₅₀ = 1.58 μM) and FGFR-1 (IC₅₀ = 1.6 μM). SU10944 selectively inhibits VEGFR receptor downstream signaling, neovascularization, vascular permeability, VEGF-mediated tissue factor production, and induces tumor growth delay. SU10944 can be used in research related to diabetic retinopathy, exudative age-related macular degeneration or cancer.

FAM labled Ultevursen sodiumis a FAM labled Ultevursen sodium (HY-147412A). Ultevursen sodium (QR-421a) is a splice-modulating antisense oligonucleotide targeting exon 13 of the USH2A gene, which restores the functional expression of Usherin protein by inducing exon skipping. Ultevursen sodium binds to USH2A pre-mRNA and modulates the splicing process to specifically skip exon 13 carrying the pathogenic mutation c.2299delG, generating an in-frame transcript and a truncated yet functionally normal protein. Ultevursen sodium exhibits concentration-dependent exon skipping activity in human cells and retinal organoid models, and restores Usherin expression and retinal function in zebrafish and gene-edited mouse models. Ultevursen sodium can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa.

Ultevursen (QR-421a) is a splice-modulating antisense oligonucleotide targeting exon 13 of the USH2A gene, which restores the functional expression of Usherin protein by inducing exon skipping. Ultevursen binds to USH2A pre-mRNA and modulates the splicing process to specifically skip exon 13 carrying the pathogenic mutation c.2299delG, generating an in-frame transcript and a truncated yet functionally normal protein. Ultevursen exhibits concentration-dependent exon skipping activity in human cells and retinal organoid models, and restores Usherin expression and retinal function in zebrafish and gene-edited mouse models. Ultevursen can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa.

ANX-M1 is a blood-brain barrier-permeable anti-C1q antibody. ANX-M1 can slow down the progression of retinal degeneration following photo-oxidative damage. ANX-M1 has been incorporated into nanocarriers to evaluate its brain delivery efficacy in a mouse model of Alzheimer's disease. ANX-M1 is applicable for research on age-related macular degeneration and Alzheimer's disease ^[1].

Aminoguanidine (Pimagedine) hemisulfate is an inhibitor of diamine oxidase (DAO) and nitric oxide synthase (NOS). Aminoguanidine hemisulfate can reduce the formation of advanced glycation end products (AGEs). Aminoguanidine hemisulfate has a dose-dependent inhibitory effect on Doxorubicin (HY-15142)-induced cell apoptosis. Aminoguanidine hemisulfate has antioxidant properties. Aminoguanidine hemisulfate can be used in the research of diabetic nephropathy.

Fluoflavine (ML-090) is a selective NOX1 inhibitor and reactive oxygen species inhibitor. Fluoflavine reduces reactive oxygen species production, NOX1-mediated downstream signaling events, and oxygen-glucose deprivation-induced retinal ganglion cell death. Fluoflavine inhibits NADPH oxidase activity and pathological retinal neovascularization induced by oxygen-induced retinopathy in the retinas of ischemic mice. Fluoflavine can be used in studies related to retinal ischemia-reperfusion injury and proliferative retinopathy.

Avacincaptad pegol (Izervay) is a selective inhibitor targeting complement component C5, and is a pegylated ribonucleic acid aptamer. Avacincaptad pegol inhibits the cleavage of C5 into pro-inflammatory C5a and C5b, which forms the membrane attack complex (C5b-9), thereby reducing inflammatory cell recruitment and retinal cell damage. Avacincaptad pegol can slow the growth of geographic atrophy (GA) lesions and reduce the risk of persistent vision loss. Avacincaptad pegol can be used in research of geographic atrophy associated with age-related macular degeneration (AMD) and has been approved by the FDA.

PG-901 is a full, selective MC5R agonist (EC₅₀ = 0.072 nM for hMC5R). PG-901 is also a full antagonist at the hMC3R and the hMC4R (K_b: 1.0 nM and 0.53 nM, respectively). PG-901 significantly diminishes Cytokines (IL-1α, IL-1β, IL-6). PG-901 increases glucose tolerance, reduces blood glucose, decreases retinal damage.

S-Ac7-DOG is a cationic lipid with biodegradability, low immunogenicity and high nucleic acid transfection capacity, which is commonly used to construct lipid nanoparticles for nucleic acid molecule delivery. S-Ac7-DOG can bind to mRNA, microRNA and self-amplifying RNA through electrostatic interaction. Lipid nanoparticles formed by S-Ac7-DOG enter cells via an energy-dependent endocytic pathway, release nucleic acid cargos, induce antigen-specific CD8⁺ T cell responses, promote the generation of precursor memory T cells, and regulate neuroinflammatory pathways. S-Ac7-DOG can be used in the research of retinal diseases, neuroinflammation and cancer.

Ultevursen sodium (QR-421a) is a splice-modulating antisense oligonucleotide targeting exon 13 of the USH2A gene, which restores the functional expression of Usherin protein by inducing exon skipping. Ultevursen sodium binds to USH2A pre-mRNA and modulates the splicing process to specifically skip exon 13 carrying the pathogenic mutation c.2299delG, generating an in-frame transcript and a truncated yet functionally normal protein. Ultevursen sodium exhibits concentration-dependent exon skipping activity in human cells and retinal organoid models, and restores Usherin expression and retinal function in zebrafish and gene-edited mouse models. Ultevursen sodium can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa.

Aminoguanidine (Pimagedine) is an inhibitor of diamine oxidase (DAO) and nitric oxide synthase (NOS). Aminoguanidine can reduce the formation of advanced glycation end products (AGEs). Aminoguanidine has a dose-dependent inhibitory effect on Doxorubicin (HY-15142)-induced cell apoptosis. Aminoguanidine has antioxidant properties. Aminoguanidine can be used in the research of diabetic nephropathy.

ANX-M1 Mouse IgG1 is a brain-penetrant C1q inhibitor. ANX-M1 Mouse IgG1 blocks classical complement pathway activation, reduces C1q concentrations in brain and plasma, and inhibits microglia-mediated synapse engulfment. ANX-M1 Mouse IgG1 can be used for the research of Huntington's disease, Alzheimer's disease, retinopathy and neuropathic pain.

Anti-CD160 Antibody (MAT 302) (CL1-R2) is a human monoclonal antibody targeting CD160. Anti-CD160 Antibody (MAT 302) blocks the CD160-HVEM protein interaction, inhibits FGF2-mediated renal tubular vascular growth, and induces endothelial cell apoptosis. Anti-CD160 Antibody (MAT 302) targets CD160 on neovascularization to exert anti-angiogenic and vascular normalization effects, trigger the production of IFN-γ, TNF and IL-6 by NK cells, and enhance glucose metabolism of NK cells through the AKT/mTOR/s6k signaling pathway. Anti-CD160 Antibody (MAT 302) reduces vascular density, normalizes remaining tumor blood vessels, and inhibits tumor growth in melanoma-bearing mice. Anti-CD160 Antibody (MAT 302) can be used in research related to neovascularization, proliferative diabetic retinopathy, and melanoma.

Norbixin is an orally active natural product with multiple activities such as retinal protection and oxidative stress regulation. Norbixin scavenges ROS, chelates metal ions, regulates plasmid and genomic DNA breakage, inhibits H₂O₂-induced mutagenesis, activates PPAR-α, modulates lipid levels, restores or regulates antioxidant enzyme activity, and alters NO levels. Norbixin prevents A2E accumulation and protects photoreceptor cells and retinal pigment epithelial cells. Norbixin is a derivative of Bixin (HY-N6884). Norbixin can be used in research related to diseases such as macular degeneration and diabetes, and also serves as a natural textile dye.