Colitis

Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC₅₀ of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC₅₀=182 nM). Necrostatin-1 is also an IDO inhibitor.

5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

Oxazolone is a haptenizing agent that induces acute or chronic inflammation of the large intestine and is used to construct models of colitis. Oxazolone can cause Th1/Th2-dependent colitis with weight loss and diarrhea. Oxazolone-induced inflammation can be mitigated by neutralizing anti-IL-4 or anti-TNF-α antibodies or decoy IL-13R2-α-FC proteins.

Apyrase is an Nucleoside triphosphate diphosphohydrolase (NTPDase). Apyrase can hydrolyze extracellular adenosine triphosphate (ATP) and adenosine diphosphate (ADP). Apyrase can inhibit Stx2 toxin release of enterohemorrhagic Escherichia coli (EHEC) infection and protect the intestinal barrier function. Apyrase can be used for the research of infection and inflammation, such as hemorrhagic colitis.

L-Isoleucine is an orally active branched chain amino acid, which is the L-enantiomer of isoleucine. L-Isoleucine has a role as a Saccharomyces cerevisiae metabolite, an Escherichia coli metabolite, a plant metabolite, a human metabolite, an algal metabolite and a mouse metabolite. L-Isoleucine regulates the inflammatory response to protect against pathogens in vivo and in vitro.

Spesolimab (BI 655130) (WT IgG1) is a mouse-derived humanized IgG1k antibody against IL-36R. Spesolimab (WT IgG1) retains the native wild-type Fc. Spesolimab (WT IgG1) is associated with a reduction in biomarkers associated with the innate, Th1/Th17 and neutrophil pathways. Spesolimab (WT IgG1) is being investigated in palmoplantar pustulosis (PPP).

GR 113808 is a potent and highly selective 5-HT₄ receptor antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors.

D-psicose is an orally active rare sugar. D-psicose inhibits p38-MAPK phosphorylation and MCP-1 expression. D-psicose inhibits the AGEs/RAGE/NF-κB pathway. D-psicose protects pancreatic β-islets, improves hyperglycemia and high-fat diet-induced non-alcoholic fatty liver disease.

Dextran sulfate sodium salt (DSS) (MW 35000-45000) is a polymer of dehydrated glucose with a molecular weight of approximately 35000-45000. DSS with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (DSS) (MW 35000-45000) is a potent inducer of colitis. Dextran sulfate sodium salt (DSS) (MW 35000-45000) can be used to induce model acute colitis, chronic colitis, and colitis-related colon cancer. Dextran sulfate sodium salt (DSS) (MW 35000-45000) may be related to macrophage dysfunction, intestinal flora dysbiosis, and is particularly toxic to the colonic epithelium.

Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.

Rosnilimab (ANB030) is a PD-1 agonist IgG1 monoclonal antibody. Rosnilimab can inhibit T cell proliferation, the secretion of inflammatory cytokines, and reduce CD4 and CD8 T cells with high PD-1 expression. Rosnilimab can be used in the research of inflammatory diseases such as colitis and rheumatoid arthritis.

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

Hippuric Acid is an orally active metabolite. Hippuric Acid can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Hippuric Acid decreases NRF2, MMP9 and leads to ROS accumulation. Hippuric Acid activates TGFβ/SMAD signaling. Hippuric Acid improves hyperuricemia and colitis. Hippuric Acid can also be used in cardiovascular disease research. .

Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a glucocorticoid, is an orally active steroidal anti-inflammatory agent (SAID) with anti-inflammatory and immunomodulatory activities. Hydrocortisone hemisuccinate inhibits the bioactivity of IL-6 and IL-3 with IC₅₀ values of 6.7 and 21.4 μM, respectively. Hydrocortisone hemisuccinate can be used in the study of ulcerative colitis (UC) and recurrent oral ulcers.

Glycolithocholic acid (Lithocholylglycine), an endogenous metabolite, is a glycine-conjugated secondary bile acid. Glycolithocholic acid can be used to diagnose ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH) and primary sclerosing cholangitis (PSC).

Fmoc-Leucine (N-FMOC-leucine) is an anti-inflammatory agent that not only promotes extracellular Ca²⁺ influx but also facilitates intracellular Ca²⁺ release. Fmoc-Leucine is a selective ligand for PPARγ (K_i = 15 μM), exhibiting insulin-sensitizing effects but with weak fatogenic activity. Fmoc-Leucine exhibits unique self-assembly properties and can form transient gels, stable gels, or crystals/2D sheets through different pathways. Fmoc-Leucine can be used in the research of diabetes, colitis, and bladder cancer.

Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

Sodium acetate trihydrate, 99.5% is a carboxylic acid and short-chain fatty acid (SCFAs). Sodium acetate trihydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Sodium acetate trihydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Sodium acetate trihydrate regulates energy metabolism. Sodium acetate trihydrate has anticancer activity against gastric cancer. Sodium acetate trihydrate induces writhing reaction and ulcerative colitis. Sodium acetate trihydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.

Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.

PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC₅₀=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC₅₀=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.