anti-ulcerative

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].

Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.

18β-Glycyrrhetinic acid (Enoxolone) is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.

Hydrocortisone hemisuccinate (hydrocortisone 21-hemisuccinate*free acid) is a corticosteroid used as an analytical and chromatography reagent.

Olsalazine disodium (Dipentum) is bioconverted to 5-aminosalicylic acid (5-ASA) in the colon and has anti-inflammatory activity in ulcerative colitis.

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.

MoTPS1-IN-1 is a potent MoTPS1 inhibitor with antifungal and potentially anti-inflammatory activity that acts through interaction with Glu396 and can be used to study ulcerative colitis.

Dersalazine (Dersalazine Free Base), an inhibitor of platelet-activating factor, exerts intestinal anti-inflammatory activity in different rodent types of colitis by down-regulating IL-17 expression, with potential efficacy in patients with ulcerative colitis.

Anti-inflammatory agent 92 (compound LD4), a porphyrin derivative, exhibits anti-inflammatory properties. It alleviates ulcerative colitis by inhibiting the STAT3-EPHX2 axis.

Olsalazine (Dipentium), an anti-inflammatory drug, is used in the treatment of inflammatory bowel disease. It is also a novel DNA hypomethylating agent.

Anrukinzumab (IMA-638), a humanized anti-IL-13 monoclonal antibody, effectively reduces lung inflammation in cynomolgus monkeys and shows potential in the studies of ulcerative colitis (UC) and asthma [1] [2] [3].

Anti-inflammatory agent 51 is an amide sulfonamide derivative with anti-inflammatory and potentially anti-tumor activity and inhibition of NF-κB activation, which can be used to study acute lung injury and ulcerative colitis.

Hydrocortisone hemisuccinate hydrate (Hydrocortisone 21-hemisuccinate hydrate) is a glucocorticoid that serves as an orally active steroidal anti-inflammatory drug (SAID). It inhibits the bioactivity of IL-6 and IL-3 with IC50 values of 6.7 and 21.4 μM, respectively. This compound is applicable in research on ulcerative colitis (UC).

Dersalazine, a PAF antagonist and TNFα inhibitor, is used potentially for the treatment of ulcerative colitis. It showed anti-inflammatory effect in reactivated colitis in rats, as evidenced by a significant reduction in MPO activity.

Antimicrobial agent-21 is a potent mitogen activated protein kinase inhibitor with antibacterial, anti-inflammatory and antitumor activity for the treatment of cataracts, ulcerative colitis, meningitis and Kawasaki's disease and Parkinson's disease.

1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Gentianella acuta, exhibiting antispasmodic and anti-inflammatory activities. Dimethylbellidifolin shows mutagenicity in Salmonella typhimurium TA100, TA98, TA97, and TA2637 by the preincubation method and significantly inhibits the growth of Staphylococcus aureus at a dose of 200 µg disk.

Tesnatilimab is a potent humanized IgG4 monoclonal antibody that binds to the immune-activating receptor NKG2D. Tesnatilimab has potential immunomodulatory and anti-inflammatory activity and can be used to study active ulcerative colitis.

Eldelumab (BMS-936557) is a humanized anti-IP-10 IgG type 1 monoclonal antibody with inhibitory activity against CXCL10. It has anti-inflammatory properties, selectively binds to CXCL10, and can be used in the study of rheumatoid arthritis, ulcerative colitis, and Crohn's disease.

Visilizumab, a humanized IgG2 monoclonal antibody with low Fc receptor binding affinity, targets the CD3 epsilon (CD3ε) subunit. It is utilized in research related to ulcerative colitis and Crohn's disease [1].

Delmitide acetate (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory properties, suppressing TNF-α, IFN-γ, and interleukin (IL)-12 production, while enhancing heme oxygenase 1 activity. It is utilized in research related to ulcerative colitis [1] [2].

Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)

Metyrosine (α-Methyltyrosine) is an antihypertensive drug and could be used as a tyrosine hydroxylase inhibitor.Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.

Elucaine is an antagonist of the muscarinic acetylcholine receptor. It has anti-ulcerative activity.