dysfunction

VBIT-4 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 17 μM). VBIT-4 can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Alfuzosin (SL 77499) is an orally available, competitive α1-adrenoceptor antagonist.Alfuzosin induces smooth muscle relaxation in the bladder neck and prostate.Alfuzosin has been used to study benign prostatic hypertrophy, lower urinary tract symptoms (LUTS), and ejaculatory dysfunction (EjD).

CGP 3466B maleate (Omigapil maleate) is an orally bioavailable GAPDH nitrosylation inhibitor. Omigapil maleate abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD).

3-Aminobenzamide (PARP-IN-1) is an effective inhibitor of PARP (IC50<50 nM in CHO cells) and a mediator of oxidant-induced myocyte dysfunction during reperfusion.

CP 866087 is an opioid receptor antagonist for the study of female sexual dysfunction.

Chloranil (tetrachloro-p-benzoquinone) triggers inflammation and neurological dysfunction through Toll-like receptor 4 signaling and can be used to model inflammation in mice.

geraniol provides a potent protective effect against cardiac dysfunction induced by diabetes. This ameliorative effect could be attributed to its suppression of oxidative stress.

Triheptanoin (IND 106011) is a fatty acid metabolic modulator. It potentially for the treatment of fatty acid oxidation disorders and GLUT1.

CP-866087 is a novel, potent and selective mu-opioid receptor antagonist for the study of female sexual dysfunction.

1. Oxyresveratro can inhibit tyrosinase activity. 2. Oxyresveratro is useful to trauma models, as toxicity to glia could be beneficial by inhibiting reactive gliosis. 3. Oxyresveratrol (trans-Oxyresveratrol) has antioxidant activity, can reduce neuronal oxidative damage and protect hepatocytes against oxidative stress and mitochondrial dysfunction, which may be associated with activation of Nrf2.

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

CBS-1114 HCl (N-Phenylbenzamidrazone hydrochloride) is a 5-lipoxygenase inhibitor and an anti-inflammatory compound in a good eye-permeable model.CBS-1114 HCl maintains and improves cardiac function, attenuates cardiac dysfunction, as well as reduces epicardial adipose tissue and/or pericardial adipose tissue in subjects with cardiovascular disease.

MK-0533 is a novel PPARγ partial agonist for the prevention of vascular endothelial dysfunction (VED) and VED-related cardiovascular disease.

TT01001 (Ethyl 4-(3-(3,5-dichlorophenyl)thioureido)piperidine-1-carboxylate) is a selective agonist of mitoNEET and reduces oxidative stress injury and neuronal apoptosis by improving mitochondrial dysfunction. TT01001 can be used in studies about the treatment of type II diabetes.

Fipamezole is a potent alpha2 adrenergic receptor antagonist that may be useful for studying autonomic dysfunction in Parkinson's disease.

Dalzanemdor (SAGE-718) is an NMDA receptor-positive modulator of metabolism that can be used to study Huntington's chorea, Alzheimer's disease, and cognitive dysfunction.

Flurochloridone (R 40244) is a selective herbicide. Flurochloridone induces apoptosis and is regulated by mitochondrial dysfunction and oxidative stresses.

DL-Syringaresinol ( (±)-Syringaresinol) is a lignan from ginseng berries with anti-inflammatory, antioxidant, analgesic and weak anti-mycobacterial activities.DL-Syringaresinol can delay oxidative stress-induced skin aging through autophagy, alleviate oxaliplatin-induced neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses. neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses.

Binospirone (MDL 73005EF) is a 5-HT1A receptor agonist with anxiolytic activity used in the study of glaucoma and movement disorders associated with neurologic dysfunction.

Rovatirelin (S-0373) is a newly synthesized thyrotropin-releasing hormone (TRH) analog that ameliorates cytosine arabinoside-induced motor dysfunction in a rat model of spinal cerebellar degeneration via acetylcholine and dopamine neurotransmission.

GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

SXC 2023 ((S)-2-acetamido-3-(4-methylbenzoylthio)propanoic acid) is a therapeutic prodrug of N-acetyl-L-cysteine for the treatment of CNS disorders and neurocognitive disorders, and can be used to treat glutamatergic dysfunction and psychiatric disorders in which oxidative stress plays a key role.

Anti-inflammatory agent 49 is a potent inhibitor of Drp1-Fis1 interaction, inhibits GTPase, and can be used in the study of diseases caused by mitochondrial dysfunction.

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.OR-1896 can be used to study heart failure and vascular dysfunction. OR-1896 can be used to study heart failure and vascular dysfunction.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent, generated by the reaction of linoleic acid with plant and mammalian lipoxygenases, and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid inhibits the adhesion of tumor cells to the vascular endothelium and down-regulates the expression of IRGpIIb/IIIa receptors at around 1 μM. (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX), which often acts as an endogenous ligand to activate PPARγ. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial damage.

10β,17β-dihydroxyestra-1,4-dien-3-one is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol. It alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.

RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression,has the potential for type 2 diabetes treatment. RH01386 restores ER stress-impaired glucose-stimulated insulin secretio

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase, with anti-leukemic activity, effective in endothelial dysfunction, immunosuppression, and metabolism.

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

Stemazole is a novel small molecule human stem/progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

Hydroxythiohomosildenafil (Sulfohydroxyhomo sildenafil) is a sildenafil analog that may be used to study erectile dysfunction.

Dasantafil (SCH446132) is a small molecule phosphodiesterase-5A (PDE5A) inhibitor used to treat genitourinary disorders and study erectile dysfunction.

USP30 inhibitor 11 (USP30-IN-11) is a selective USP30 inhibitor (IC50: 0.01 µΜ) that inhibits SVA and can be used in studies of cancer, mitochondrial dysfunction and Parkinson's.

Sonlicromanol hydrochloride (KH176 hydrochloride) is a ROS-redox modulator that crosses the blood-brain barrier, has potential anticancer activity, improves m.3243A>G heterogeneity in iPSC-derived neurons associated with It has potential anticancer activity, ameliorates neuronal network dysfunction and transcriptomic changes associated with m.3243A>G heterogeneity in iPSC-derived neurons, and can be used for the treatment of mitochondrial diseases.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Deferoxamine（Desferrioxamine B） is an iron chelator (binds Fe(III) and many other metal cations) that inhibits neuronopathy, may be used to modify the reduction of iron accumulation and deposition in tissues, and may improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation following traumatic brain injury.Desferrioxamin-B has antioxidant, antiproliferative, Deferoxamine has antioxidant, antiproliferative, and antitumor activities, and can induce HIF-1α production, apoptosis and autophagy in cancer cells.Desferrioxamin-B can be used in the treatment of acute iron toxicity and COVID-19 related diseases.

Luteolinidin chloride is a natural product. It is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.

Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents endothelial cell injuries from oxidized LDL via inhibition of lectin-like ox-LDL receptor-1 upregulation, interference of ox-LDL-mediated intracellular signaling pathway (p38MAPK activation, NF-kappaB nuclear translocation, eNOS expression) and the antioxidant activity of isorhamnetin. Isorhamnetin prevents endothelial dysfunction, superoxide production, and overexpression of p47phox induced by angiotensin II. Isorhamnetin appears to be a potent drug against esophageal cancer due to it's in vitro potential to not only inhibit proliferation but also induce apoptosis of Eca-109 cells.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Isolongifolene ((-)-Isolongifolene), a tricyclic sesquiterpene isolated from Murraya koenigii, exhibits antioxidant, anti-inflammatory, anticancer, and neuroprotective properties. It mitigates Rotenone-induced oxidative stress, mitochondrial dysfunction, and apoptosis by modulating the PI3K/AKT/GSK-3β signaling pathways.

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

Dextran sulfate sodium salt (MW 4500-5500) is an anhydrous glucose polymer with a molecular weight range of 4500-5500. Dextran sulfate sodium salt (MW 4500-5500) inhibits human immunodeficiency virus replication by preventing viral adsorption to host cells. Dextran sulfate sodium salt (MW 4500-5500) is a commonly used modeling compound for inflammatory bowel disease. It can destroy the integrity of the intestinal mucosal barrier through the high negative charge caused by sulfate groups, leading to intestinal barrier damage, macrophage dysfunction, and bacterial flora disorder.

Perhexiline is an orally active inhibitor of CPT1 and CPT2 that reduces fatty acid metabolism. Perhexiline can cross the blood-brain barrier (BBB) and exhibits anti-tumor activity. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatocytes. Therefore, Perhexiline can be used in cancer and cardiovascular disease research [1] [2] [5].

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

ZG36, a human Caseinolytic protease P (ClpP) agonist, non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, causing mitochondrial dysfunction and inducing leukemic cell death. Additionally, it inhibits the development of acute myeloid leukemia in a xenograft mouse model [1].

Catechin 7-O-β-D-glucopyranoside, a natural product identified in Ulmus davidiana and Paeonia obovata, demonstrates oral activity and possesses antioxidant and anti-inflammatory properties. It mitigates mitochondrial dysfunction and finds utility in the study of intestinal inflammatory diseases [1] [2] [3].