inflamed

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.

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the earliest event in acute inflammation, with equipotency to RvD1 (EC50 = ~30 nM).[3] 17(R)-RvD1 exhibits a dose-dependent reduction in leukocyte infiltration in a mouse model of peritonitis with maximal inhibition of ~35% at a 100 ng dose.[3] In contrast to RvD1, the aspirin-triggered form resists rapid inactivation by eicosanoid oxidoreductases. Analytical and biological comparisons of synthetic 17(R)-RvD1 with endogenously derived 17(R)-RvD1 have confirmed its identity as matching the natural product.[4]

ASIC blocker (IC50 values are 0.44, 2.1 μM and no effect at rat ASIC1a, ASIC3 and ASIC2a, respectively: IC50 value = 0.12 μM at human ASIC1a with no effect at ASIC2a or ASIC3). Inhibition was also observed at heteromeric ASIC channels (IC50 values are 0.79, 0.87 and 4.5 uM at rat ASIC1a+3, ASIC1a+2a and ASIC2a+3; IC5O values are 0.33 and 0.69 uM at human ASIC1a+2a and ASIC1a+3, with no effect at ASIC2a+3). Attenuates pathophysiological nociceptive behaviors in CFA-inflamed and CCI rats.

Resolvin D5 is an oxidised lipid mediator derived from docosahexaenoic acid (DHA) with anti-inflammatory properties. It inhibits the production of interleukin-6 (IL-6) and chemokine CCL5 in LPS-stimulated THP-1 cells via the ERK-NF-κB signalling pathway.

GSK2239633 is a potent CC-chemokine receptor 4 antagonist with pIC50 of 7.9. The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma pathogenesis due to its ability to recruit type 2 T-helper lymphocytes to the inflamed airways. Therefore, CCR4 provides an excellent target for anti-inflammatory therapy.

ACT-672125 is a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases. ACT-672125 showed good physicochemical properties and safety profile. In a proof-of-mechanism model of lung inflammation, ACT-672125 inhibited the recruitment of CXCR3 expressing T cells into the inflamed lung in a dose-dependent manner.

Phenylbutazone-d9 is intended for use as an internal standard for the quantification of phenylbutazone by GC- or LC-MS. Phenylbutazone is a non-steroidal anti-inflammatory drug and an inhibitor of the peroxidase activity of COX (IC50 = ~100 µM in the presence of hydrogen peroxide). It also inhibits prostaglandin I synthase (IC50 = ~25 µM in the presence of hydrogen peroxide). Phenylbutazone (2 mg kg) reduces increases in type II collagen levels in the inflamed joints of an equine model of LPS-induced acute synovitis. Formulations containing phenylbutazone have been used in the treatment of lameness in horses.

Zn-DPA-maytansinoid conjugate 1, a small molecule-based immune checkpoint-targeting maytansinoid conjugate, effectively induces sustained tumor growth regression and transforms the tumor microenvironment (TME) into an inflamed hot tumor [1].

TOP1288 is a narrow-spectrum kinase inhibitor targeting P38α, Src, and Syk kinases, with IC 50 values of 116nM, 24nM, and 659nM, respectively. It effectively inhibits inflammatory cytokine release from inflamed biopsies and myofibroblasts [1].

F11R peptide TFA is a molecule of the F11 receptor. It inhibits platelet aggregation induced by anti-F11R antibodies and prevents platelet adhesion to endothelial cells inflamed by cytokines (TNFα and INF-γ). F11R peptide TFA is applicable in research on atherosclerotic plaques and related thrombotic diseases.

Hyaluronan-binding peptide, biotin labeled TFA, is a bioactive peptide. (This peptide is biotinylated through a C-terminal GGGSK spacer and binds to hyaluronan. Hyaluronan (HA) is a non-sulfated glycosaminoglycan found in the extracellular matrix and on cell surfaces. It plays a significant role in fertilization, embryonic development, wound healing, angiogenesis, leukocyte transport to inflamed tissues, and cancer metastasis. This peptide has been demonstrated to block the interaction between HA and CD44 receptors and inhibit T-cell proliferation.)