Ulcerative Colitis

γ-Glu-Tyr is an orally active gut microbiota-derived metabolite and a competitive DPP-IV inhibitor with an IC₅₀ of 6.77 mM against hDPP-IV. γ-Glu-Tyr weakly activates hCaSR. γ-Glu-Tyr decreases colonic pro-inflammatory cytokine (IL-6, IL-1β, TNF-α) levels. γ-Glu-Tyr activates the cAMP/PKA signaling pathway and inhibits NF-κB phosphorylation, thereby reducing inflammatory responses. γ-Glu-Tyr can be used for research on type 2 diabetes and ulcerative colitis.

CPA inhibitor (Compound 5) (Carboxypeptidase inhibitor) is an orally active competitive carboxypeptidase A (CPA) inhibitor with a K_i value of 0.32 μM. CPA inhibitor blocks the activity of carboxypeptidase A3 (CPA3). CPA activator activates the Wnt/Lrp6/β-catenin signaling pathway. CPA inhibitor reduces epithelial damage. CPA inhibitor is applicable to research related to inflammatory bowel disease, including ulcerative colitis and Crohn's disease.

5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.

Melredableukin alfa (RG7835) is a bivalent conjugate composed of a human IL-2 mutant (T3A, N88D, C125A) and human IgG1. Melredableukin alfa exhibits enhanced Treg cell selectivity in cynomolgus monkey and humanized mouse models. Melredableukin alfa can be used in research related to ulcerative colitis and autoimmune hepatitis.

Linderane is an orally active natural sesquiterpene lactone with blood-brain barrier permeability. Linderane indirectly activates PDE3 by activating ERK/STAT3, thereby inhibiting the cAMP/PKA/CREB signaling pathway and hepatic gluconeogenesis. Linderane protects pancreatic β cells against oxidative damage by inhibiting the activation of the p38 MAPK pathway and activating the Nrf2 pathway. Linderane inhibits cell apoptosis and ameliorates intestinal mucosal inflammation by suppressing the IL-6/JAK/STAT3 signaling pathway. Linderane reduces pain sensitivity and alleviates anxiety-like behaviors by activating cannabinoid receptor 2 (CB2R). Linderane can be used in studies related to type 2 diabetes, ulcerative colitis, and chronic inflammatory pain with anxiety.

2,4-Dinitrobenzenesulfonic acid (DNBS; DNBSO) sodium salt (Sodium 2,4-dinitrobenzenesulfonate) is a classic colitis inducer that relies on activation of the NF-κB p65/COX-2/p38 pathway. As a hapten, 2,4-Dinitrobenzenesulfonic acid sodium salt stimulates the production of immune responses in colonic tissues, triggers oxidative stress and inflammatory reactions, and thereby leads to colonic injury. 2,4-Dinitrobenzenesulfonic acid sodium salt successfully induces models of colitis and ulcerative colitis in rats, causing pathological changes such as ulcers, edema, stenosis, shortening and organ adhesion in the distal colon, along with significant increases in the levels of inflammatory indicators and endoplasmic reticulum stress marker proteins. 2,4-Dinitrobenzenesulfonic acid sodium salt is widely used in studies on the mechanisms related to colitis and ulcerative colitis.

Licoflavone B is an orally active flavonoid, with IC₅₀ values of 23.78 μM and 31.5 μM against SmATPase and SmADPase of Schistosoma mansoni, respectively. Licoflavone B selectively targets viral RdRp, inhibits viral replication, and reduces the expression levels of viral NP and PB2. Licoflavone B inhibits c-Myc expression and suppresses cancer cell proliferation. Licoflavone B disrupts the tegument of worms, reduces egg production, and induces the death of adult Schistosoma mansoni. Licoflavone B blocks the activation of the MAPK pathway, maintains colonic barrier integrity, inhibits colonic cell apoptosis, and reshapes the gut microbiota. Licoflavone B can be used in research related to influenza, multiple myeloma, schistosomiasis, and ulcerative colitis.

Nigakinone is an orally active FXR agonist and NLRP3 inhibitor. Nigakinone suppresses bile acid-induced inflammation and cell damage, regulates the bile acid profile, and alleviates intestinal mucosal barrier injury. Nigakinone synergizes with Irinotecan (HY-16562) to inhibit the proliferation and migration of colorectal cancer cells as well as the growth of subcutaneous xenograft tumors. Nigakinone can be used in research related to ulcerative colitis and colorectal cancer.

Acloproxalap (ADX-629) is an orally active reactive aldehyde species (RASP) inhibitor. Acloproxalap binds covalently to free aldehydes, sequesters reactive aldehyde species, malondialdehyde, acetaldehyde and preformed malondialdehyde-acetaldehyde adducts, and reduces elevated RASP levels. Acloproxalap decreases the formation of aldehyde adducts, reduces liver and serum triglyceride levels, hepatic fat accumulation, circulating anti-malondialdehyde-acetaldehyde adduct antibody levels, and inhibits the release of IL-6 and MCP-1. Acloproxalap improves cell viability of liver slices exposed to ethanol. Acloproxalap blocks ethanol-induced damage in animal models of alcoholic liver disease. Acloproxalap is applicable to research related to alcoholic liver disease, alcoholic fatty liver disease, non-alcoholic steatohepatitis, chronic cough, rheumatoid arthritis, ulcerative colitis and mild atopic asthma.

Agrimonolide is a phenethyl isocoumarin compound discovered from Agrimonia pilosa, exhibiting anti-inflammatory, antioxidant, and anticancer activities. Agrimonolide inhibits NF-κB, MAPK, and TLR4-mediated neuroinflammatory signaling, suppresses Notch and JAK2/STAT3 signaling to modulate Th17/Treg balance and maintain the intestinal barrier. Agrimonolide decreases HIF1A expression, inhibits glycolysis, and induces ferroptosis and cell cycle arrest via the mTOR pathway in tumor models, thereby suppressing cancer cell viability, proliferation, and metastasis. Agrimonolide exerts hepatoprotective and anti-fibrotic effects by regulating bile acid transporter expression and reducing hepatic bile acid accumulation. Agrimonolide is used for research on ulcerative colitis, ovarian cancer, non-small cell lung cancer, cholestatic liver injury, and neuroinflammation.

Rosnilimab (Mouse IgG2a) is a mouse-derived IgG2a antibody, Rosnilimab. Rosnilimab is a PD-1 agonistic monoclonal antibody. Rosnilimab (Mouse IgG2a) optimizes the inhibitory PD-1 signaling pathway without blocking PD-L1 binding; it also activates moderately activated PD-1⁺ T cells and eliminates PD-1^high cells, Tfh/Tph cells and Teff cells. Rosnilimab (Mouse IgG2a) reduces the secretion and gene expression of IFN-γ, CXCL13, IL-6 and TNF, decreases macrophage infiltration, and downregulates the gene expression of inflammatory myeloid cells. Rosnilimab (Mouse IgG2a) can be used in studies related to ulcerative colitis.

Physalin B is an orally active anti-inflammatory and anticancer agent. Physalin B can be isolated from Physalis alkekengi L. var. Franchetii. Physalin B inhibits the activation of the NF-κB, NLRP3 inflammasome, STAT3, PI3K/Akt and Hedgehog signaling pathways, regulates the phosphorylation levels of GSK-3β, p38 MAPK, ERK1/2 and JNK, and promotes the nuclear translocation of NRF2. Physalin B reduces the levels of pro-inflammatory cytokines and factors, induces mitochondrial reactive oxygen species (mito-ROS) production, Apoptosis, G2/M cell cycle arrest and incomplete Autophagy, alters cytoskeleton structure and alleviates oxidative stress. Physalin B reduces cancer cell viability, ameliorates liver and lung tissue damage and alleviates liver fibrosis. Physalin B can be used in research related to ulcerative colitis, breast cancer, acute lung injury, colon cancer, non-alcoholic steatohepatitis, liver fibrosis, lung cancer, pancreatic cancer, lymphoma, ovarian cancer, sarcoma and leukemia.

LY237 is a potent GPR84 full agonist, with EC₅₀ values of 0.189 nM and 0.07 nM in cAMP inhibition assay and calcium flux assay, respectively. LY237 binds to the amphipathic orthosteric pocket of GPR84, stabilizes the active conformation of the receptor, and promotes its coupling with Gαi protein. LY237 can be used in research related to ulcerative colitis, fibrotic diseases, non-alcoholic steatohepatitis, and acute respiratory distress syndrome.

Cisapride (R 51619) monohydrate is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride monohydrate also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride monohydrate exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride monohydrate can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

Camylofine is an antispasmodic agent with myogenic and neurogenic effects. Camylofine exhibits mild anticholinergic activity and blocks the M3 receptors on colonic smooth muscle. Camylofine dihydrochloride inhibits phosphodiesterase, elevates intracellular cAMP levels and reduces intracellular Ca²⁺ levels, thereby promoting smooth muscle relaxation. Camylofine can be used in studies related to antispasmodia, gastrointestinal smooth muscle and ulcerative colitis.

GE1111 is a MRGPRX2 antagonist (IC₅₀ = 9.4 μM). GE1111 inhibits MRGPRX2/MRGPRB2-mediated mast cell activation. GE1111 reduces the expressions of TSLP, IL-13, MCP-1, TNF-α, IL-1β and periostin, maintains the expression levels of claudin 1 and involucrin, restores the phagocytic activity of macrophages, and attenuates the activation of STIM1 and phosphorylated AKT. GE1111 exerts anti-inflammatory and anti-allergic effects in multiple animal models. GE1111 is applicable to the research related to rosacea, atopic dermatitis and ulcerative colitis.

Acetic acid-d₃ sodium is the deuterium labeled Acetic acid (HY-Y0319). Acetic acid is a carboxylic acid and short-chain fatty acid (SCFAs). Acetic acid activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Acetic acid exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Acetic acid regulates energy metabolism. Acetic acid has anticancer activity against gastric cancer. Acetic acid induces writhing reaction and ulcerative colitis. Acetic acid can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.

Diplacone is an orally active geranyl flavanone. It is isolated from the fruits of Paulownia tomentosa. Diplacone reduces COX-2 levels and increases the pro-MMP2/MMP2 ratio. It induces ferroptosis-mediated cell death. Diplacone enhances mitochondrial Ca²⁺ influx and ROS production. It possesses anti-inflammatory and free radical-scavenging activities. Diplacone can be used in research related to ulcerative colitis and non-small cell lung cancer.

HW201877 enantiomer is the enantiomer of HW201877 (HY-174990) and is 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitor with an IC₅₀ of 12.2 nM. HW201877 enantiomer can be used for the research of inflammatory bowel disease, idiopathic pulmonary fibrosis, ulcerative colitis, and Crohn's disease.

Minokitug is a humanized monoclonal antibody targeting the CCR2 protein. Minokitug can be used for the research of refractory/relapsed ulcerative colitis.