Colitis

N-Oleoyl-L-phenylalanine is a long-chain N-acyl-L-phenylalanine and also a mitochondrial uncoupler. N-Oleoyl-L-phenylalanine uncouples UCP1-independent respiration in mitochondria, thereby helping to regulate glucose homeostasis. As an endogenous metabolite, the level of N-Oleoyl-L-phenylalanine increases in patients with ulcerative colitis after a high-fat diet. N-Oleoyl-L-phenylalanine can be used in studies related to ulcerative colitis.

PVA (Polyvinyl alcohol) (Mw 205000) is a polyvinyl alcohol with a molecular weight of 205000, which is used as a biological additive. PVA (Mw 205000) can be cross-linked through physical or chemical methods to form hydrogels, and is widely applied in fields such as biomedicine, food packaging, textiles, papermaking, sensing, and electronic devices. After PVA enema, it has an improving effect on acute colitis induced by DSS (HY-116282C) in mice.

Roquinimex (Linomide) is an orally active immunomodulator with antineoplastic, anti-inflammatory, and antiangiogenic activity. Roquinimex suppresses TH1 lymphocyte cytokines (IL-2, IFN-γ), promotes TH2 lymphocyte cytokines (IL-4, IL-10), increases NK cell, activated monocyte, and T cell activity. Roquinimex blocks macrophage TNF-α production and suppresses IL-1/IL-6 secretion. Roquinimex exhibits in vivo antitumour activity, suppresses rodent autoimmune disease signs, and ameliorates murine colitis and psoriasis. Roquinimex can be used for the research of leukemia, inflammatory bowel disease, multiple sclerosis, and psoriasis.

Mesalazine impurity 2 is an impurity of Mesalazine (HY-15027). 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).

Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with K_i^app values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury.

Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia.

PROTAC JAK1/2 degrader-1 is an orally active JAK1/JAK2 PROTAC degrader, with DC₅₀ values of 1.4 μM and 0.92 μM against JAK1 and JAK2, respectively. PROTAC JAK1/2 degrader-1 triggers degradation via a CRBN- and proteasome-dependent pathway. PROTAC JAK1/2 degrader-1 inhibits the secretion of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). PROTAC JAK1/2 degrader-1 alleviates inflammatory responses and colon injury by inhibiting the JAK/STAT3 signaling pathway. PROTAC JAK1/2 degrader-1 can be used for the research of inflammatory bowel disease.

Lauroyl-L-carnitine-d₉ chloride is the deuterium labeled Lauroyl-L-carnitine chloride (HY-130321). Lauroyl-L-carnitine chloride is an orally active metabolite. Lauroyl-L-carnitine chloride significantly reverses the decrease in its target gene IL-10. Lauroyl-L-carnitine chloride alleviates Crohn' s-like colitis.

Lauroyl-L-carnitine-d₃ (chloride) is the deuterium labeled Lauroyl-L-carnitine chloride (HY-130321). Lauroyl-L-carnitine chloride is an orally active metabolite. Lauroyl-L-carnitine chloride significantly reverses the decrease in its target gene IL-10. Lauroyl-L-carnitine chloride alleviates Crohn' s-like colitis.

Pinobanksin is an antioxidant and anti-ferroptosis agent found in sunflower honey and propolis, with oral activity. Pinobanksin enhances Nrf2-mediated antioxidant defense, inhibits NF-κB inflammation, and suppresses apoptosis and ferroptosis in in vivo models and normal cells. Pinobanksin exhibits apoptosis-inducing effects on B-cell lymphoma cells. Pinobanksin can be used in research related to perfluorooctane sulfonate-induced renal/cardiac toxicity, acute colitis, and B-cell lymphoma.

JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis.

CP-96,345 is a non-peptide selective NK-1 receptor antagonist (K_i = 0.31 nM). CP-96,345 inhibits cell rolling, adhesion, and plasma extravasation, and inhibits degranulation and pancreatic MPO activity. CP-96,345 attenuates neurogenic inflammation, edema, and adhesion molecule expression. CP-96,345 attenuates static contraction- and muscle stretch-evoked pressor reflexes through blockade of NK-1 receptors in the dorsal horn. CP-96,345 impairs post-ischemic recovery of LVDevP, HR, and CF in isolated hearts and increases reperfusion fibrillation. CP-96,345 can be used for research on chronic colitis, myocardial ischemia-reperfusion injury, smoke inhalation and burn injury, acute pancreatitis, oxazolone colitis, and neurogenic inflammation.

JAK1/2 ligand 1 is a ligand for the PROTAC target protein of JAK1/2, which can be used to synthesize PROTAC JAK1/2 degrader-1 (HY-179715). JAK1/2 ligand 1 is applicable to the research of colitis.

Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis.

Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC₅₀ of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease.

Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

MC-ND-18 is an ATTEC degrader that degrades NLRP3 via the Autophagy pathway, with a DC₅₀ of 125.5 nM in THP-1 cells. MC-ND-18 exhibits anti-inflammatory activity in a DSS-induced mouse model of colitis. MC-ND-18 can be used for research on inflammatory bowel disease. MC-ND-18 consists of an NLRP3 inhibitor (HY-156121), a linker (HY-W018745), and an LC3 ligand.

7-Ketositosterol is an orally active inducer of apoptosis and ferroptosis. 7-Ketositosterol inhibits the phosphorylation of ERK1/2 and NF-κB, promotes the opening of the mitochondrial/apoptotic pathway, and induces ferroptosis in macrophages by increasing the levels of malondialdehyde, Fe²⁺ and ROS. 7-Ketositosterol upregulates the expression of gut microbiota-dependent PDLIM3, activates the p38MAPK/NF-κB signaling pathway, alters the composition of gut microbiota, increases the abundance of pathogenic bacteria, and exacerbates colitis in mice. 7-Ketositosterol can be used in studies related to breast cancer, liver cancer, and colitis.

(+)-Magnoflorine (α-Magnoflorine) is an orally active aporphine alkaloid with multiple biological activities. (+)-Magnoflorine promotes Parkin/PINK1 -mediated mitochondrial autophagy, inhibits the activation of NLRP3/Caspase-1 pathway, regulates the intestinal microbiota, and exhibits significant anti-inflammatory and immunomodulatory activities. (+)-Magnoflorine inhibits JNK and TLR4/NF-κB signaling pathways, activates Sirt1/AMPK pathway, alleviates neuronal oxidative stress and apoptosis. Magnoflorine upregulates miR-410-3p, inhibits HMGB1/NF-κB pathway, and has anti-tumor activity. (+)-Magnoflorine also has significant antifungal activity.

Izilendustat hydrochloride is a potent prolyl hydroxylase inhibitor. Izilendustat hydrochloride competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat hydrochloride can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat hydrochloride can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia.