bowel

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.

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).

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

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.

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.

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

Ipsalazide is a novel salicylazosulfapyridine analog for the treatment of inflammatory bowel disease.

MEG hemisulfate (Mercaptoethylguanidine hemisulfate) acts as a highly potent and selective suppressor of inducible NO synthase (iNOS), demonstrating EC50 values of 11.5 μM for iNOS, 110 μM for ecNOS, and 60 μM for bNOS in tissue homogenates. It is notably effective as a peroxynitrite scavenger and blocks peroxynitrite-triggered oxidative mechanisms. Furthermore, this compound offers protective benefits across various experimental inflammation prototypes, such as ischemia/reperfusion injury, hemorrhagic shock, periodontitis, inflammatory bowel disease, and both endotoxic and septic shock.

Declopramide (OXI-104) is a novel chemosensitizer with antitumor activity that induces apoptosis and can be used to study colorectal cancer and inflammatory bowel disease.

Minesapride, a novel 5-hydroxytryptamine 4 (5-HT4) receptor partial agonist, is a potential gastrointestinal prokinetic agent for the treatment of irritable bowel syndrome with constipation.

5-OxoETE (5-KETE) is a polyunsaturated fatty acid derivative, a chemokine for eosinophils and a potential biomarker for irritable bowel syndrome.

Renzapride (BRL 24924) is a mixed 5-hydroxytryptamine type 4 (5-HT4) agonist and 5-HT3 receptor antagonist.Renzapride can be used in the study of constipation-predominant irritable bowel syndrome (C-IBS).

Ticalopride is a 5-HT3 receptor agonist used in the treatment of digestive disorders, orofacial disorders, otorhinolaryngologic disorders, and may be used in the study of bulimia nervosa, gastroesophageal reflux, and irritable bowel syndrome.

Casanthranol, a concentrated mixture of anthranol glycosides from the dried bark of Rhamnus p. (cascara sagrada), is a stimulant laxative used to alleviate constipation and other medical conditions by increasing muscle contractions in the intestinal wall to facilitate bowel movements.

Clidinium bromide (Ro 2-3773) , a synthetic anticholinergic agent, has been shown in experimental and clinical researchers to have a pronounced antisecretory and antispasmodic effect on the gastrointestinal tract. It can inhibit muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve cramps or stomach spasms or abdominal due to colicky abdominal diverticulitis, pain, and irritable bowel syndrome.

Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders, with IBS being one of the most common multifactorial GI disorders. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Trimebutine is not an FDA-Approved Clinical drug, but it is available in Canada and several other international countries.

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.

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.

5-Acetylsalicylic acid (5-acetyl-2-hydroxybenzoic acid) has anti-inflammatory effects and can be used to treat inflammatory bowel disease, including ulcerative colitis, inflamed anus or rectum, and to maintain remission in Crohn's disease.

Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].

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.

Bisacodyl (Fenilaxan) is a diphenylmethane stimulant laxative used for the treatment of constipation and for bowel evacuation.