bowel

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

Zamifenacin fumarate (UK-76654 fumarate) is a potent, gut-selective antagonist of the muscarinic M3 receptor.

Dicyclomine hydrochloride is a muscarinic antagonist used as an antispasmodic and in urinary incontinence.

Tegaserod maleate (SDZ-HTF-919) is a 5-HT4 agonist manufactured by Novartis for managing irritable bowel syndrome and constipation. It was the only drug approved by the United States Food and Drug Administration for relieving abdominal discomfort, bloating, and constipation associated with irritable bowel syndrome. On March 30, 2007, the FDA requested that Novartis withdraw Zelnorm from the market due to alleged increased risks of heart attack or stroke associated with its use.

Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.

Sibofimloc (Antibiotic-202), an antibiotic compound, is used in treating bacterial infections.

Asimadoline (EMD-61753) is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM

PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM [1].

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

Propantheline bromide (Pro-Banthine) competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. An aspartic acid residue present in the N-terminal portion of the third transmembrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax the bronchial muscle and reduce tone and motility of intestinal smooth muscle.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

NS6180 is a potent and selective KCa3.1 channel inhibitor(IC50= 9 nM). It prevents T-cell activation and inflammation.

Tazofelone (LY-213829) is a NSAID used for the treatment of inflammatory bowel disease.

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

Tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate inhibit of human recombinant EGLN-1 as substrate after 20 mins by mass spectrophotometric analysis.

5-Aminosalicylic Acid (5-ASA) is a specific PPARγ agonist and also inhibits P21-activated kinase 1(PAK1) and NF-Κb. 5-Aminosalicylic Acid has anti-cancer and anti-inflammatory activities. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

Dextran sulfate sodium salt (MW 36,000–50,000) is a medium molecular weight polyanionic dextran derivative with strong intestinal epithelial permeability. It is the most commonly used agent for inducing inflammatory bowel disease (IBD) models, effectively inducing both acute and chronic colitis. Its mechanism may involve macrophage dysfunction and gut microbiota dysbiosis. Due to its colonic epithelial toxicity, long-term use can also induce colorectal cancer models.

Oxazolone is a haptenating agent that can induce models of acute or chronic colitis and atopic dermatitis. It activates Th1/Th2 responses, leading to weight loss and diarrhea, and the resulting inflammation can be alleviated by anti-IL-4 antibodies, anti-TNF-α antibodies, or IL-13R2α-Fc fusion proteins. It is also suitable for studying gene expression related to inflammatory bowel disease in zebrafish.

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

INT-777 (S-EMCA) is a potent, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.