infiltration

Oglemilast (GRC 3886) suppresses pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast is an effective and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 0.5 nM for PDE4D3). Oglemilast has the potential for inflammatory airway diseases.

S-Y048 is an Oxoeicosanoid (OXE) receptor antagonist that inhibits allergen-induced eosinophil infiltration into the skin of experimentally sensitized rhesus monkeys to house dust mites and inhibits lung inflammation caused by aerosolized allergen challenge. S-Y048 can be used to study asthma and other eosinophilic diseases.

LJP-1586 HCl, a highly selective inhibitor of vascular adhesion protein-1 (VAP-1), exhibits antiinflammation effect by reducing adhesion molecule expression and immune cell infiltration after intracerebral hemorrhage (ICH).

Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

Thioacetamide is a hepatotoxicant used widely to induce experimental liver lesions, develops hepatocellular necrosis and subsequent inflammation (mainly M1- M2-macrophages without neutrophil infiltration) in rats.

Eleutheroside E has anti-inflammatory effects by inhibiting NF-κB activities. Eleutheroside E significantly decreases the inflammatory cell infiltration, pannus formation, cartilage damage, bone erosion of CIA mice, the generation of TNF-α and IL-6, the m

Mepivacaine hydrochloride (Mepivacaine HCl) is the hydrochloride salt form of mepivacaine, an amide derivative with local anesthetic properties.

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH) inhibitor, exhibiting marked anti-inflammatory efficacy and high target selectivity.

Resolvin E1 is an effective endogenous pro-resolving mediator of inflammation. Resolvin E1 has unique counterregulatory actions that inhibit PMN transendothelial migration. Resolvin E1 also acts as an effective inhibitor of leukocyte infiltration, dendrit

Betamethasone 17-Propionate is a compound used in the study of its effects on endotoxin-induced uveitis in rats, capable of inhibiting cellular infiltration into the aqueous humor when administered topically or systemically at certain doses. However, compared to some other compounds, its inhibitory effects are relatively weaker. When administered systemically, the dosage is 1mg kg. Additionally, in in vitro interleukin-8 (IL-8) release assays, Betamethasone 17-Propionate's suppression of IL-8 release from rat peritoneal exudate cells is less effective than that of betamethasone. Moreover, the concurrent addition of betamethasone dipropionate with Betamethasone 17-Propionate reduces the suppressive effects of betamethasone on cell infiltration and IL-1β gene expression.

TAK-661 is an inhibitor of eosinophil chemotaxis (eosinophil chemotaxis) that significantly alleviates late-phase bronchoconstriction while inhibiting the proliferation of eosinophils in bronchoalveolar lavage (BAL) and their infiltration into the airway walls.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

NeoSTX (Neosaxitoxin) is a specific sodium channel blocker that targets site 1. It works synergistically with local anesthetics to provide surgical anesthesia through peripheral nerve block or local infiltration and significantly prolongs postoperative analgesia duration.

Anti-NASH agent 2 (compound 21) is an inhibitor of neolipogenesis activity and α-SMA gene expression. It improves hepatic steatosis, edema, inflammatory infiltration, and liver fibrosis in NASH mouse models.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.

Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and exhibits low oral bioavailability. By inhibiting cGAMP degradation, it effectively activates the intracellular STING pathway. Enpp-1-IN-25 can enhance immune cell infiltration and type I interferon response in the tumor microenvironment, thereby increasing the antitumor efficacy of anti-PD-L1 antibodies. It is applicable for research in cancer immunotherapy.

PD-L1 HDAC-IN-1 (Compound 14) is an inhibitor of PD-L1 and HDAC, effectively blocking PD-1 PD-L1 interaction as well as HDAC2 and HDAC3 with IC50 values of 88.10, 27.98, and 14.47 nM, respectively. It exhibits mild cytotoxicity in MCF-7 cells (IC50=19.34 μM) and enhances the expression of PD-L1 and CXCL10, promoting antitumor immune responses by recruiting T cell infiltration into the tumor microenvironment (TME).

JAK1 STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1 STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1 STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1 JAK1 and p-STAT3 STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).

P2Y14 antagonist 1 (compound 45) is a highly selective and orally active P2Y14 receptor antagonist with an IC50 value of 0.70 nM. It demonstrates significant anti-inflammatory effects by effectively reducing pulmonary infiltration of immune cells and inflammatory responses through the inhibition of the NLRP3 signaling pathway. P2Y14 antagonist 1 is suitable for studying acute lung injury.

IDT is an orally active TNFα modulator. It acts by altering neutrophil infiltration, improving cognition and diminishing tau and amyloid pathology in the 3xTgAD mouse model.

TCV-309 is an inhibitor of platelet activating factor (PAF). TCV-309 reduces graft PMN infiltration and enhances early function of 24-hour-preserved rat kidneys with long warm ischemia. TCV-309 attenuates the priming effects of bronchoalveolar macrophages

AUY-954 is an effective selective S1P(1) modulator. It can significantly reduce the local expression of EAN rat sciatic nerve T cells, B cells, macrophage infiltration, inflammatory demyelination, interleukin-17 and matrix metalloproteinase-9.