swelling

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.

Zoniporide hydrochloride is a selective inhibitor of NHE-1 with IC50 of 14 nM which is >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride shows an IC50 of 59 nM for NHE-1-dependent swelling of human platelets.

S-(+)-Ketoprofen ((S)-(+)-Ketoprofen) works by blocking the action of a substance in the body called cyclo-oxygenase. It belongs to a class of medicines called non-steroidal anti-inflammatory drugs (NSAIDs). Cyclo-oxygenase is involved in the production of chemicals in the body called prostaglandins. Prostaglandins are produced in response to injury or certain diseases and would otherwise go on to cause swelling, inflammation and pain. By blocking cyclo-oxygenase, S-(+)-Ketoprofen prevents the production of prostaglandins and therefore reduces inflammation and pain. Along with Peripheral analgesic action it possesses central analgesic action.S-(+)-Ketoprofen is a non-steroidal anti-inflammatory drug. It is manufactured by Menarini, under the tradename Keral. It is available in the UK, as S-(+)-Ketoprofen trometamol, as a prescription-only drug and in Latin America as Miracox, produced by Stein in Costa Rica. In Italy it is available as an over the counter-drug under the tradename Enantyum. In Lithuania it is available as over the counter-drug uder tradename Dolmen.

Pamabrom is a diuretic, used for the relief of temporary water weight gain, bloating, swelling and full feeling associated with the premenstrual and menstrual periods.

Diflucortolone valerate (Diflucortolone 21-valerate) is a corticosteroid esterified with valeric acid. It helps to reduce itching, redness, and swelling.

AN3485 Hydrochloride is a novel anti-inflammatory agent and Toll-like receptor (TLR) inhibitor. It can reduce PMA-induced ear swelling and is used in dermatological research.

Peptide5 acetate reduces animal swelling, astrogliosis, and neuronal cell death after spinal cord injury. Peptide5 acetate significantly reduces the degree of spinal cord injury (SCI) in a rodent ex vivo model.

Agaricic acid is an adenine nucleotide translocase antagonist.It is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid (Agaricinic Acid) induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism.

BI-9627 is a selective and potent sodium hydrogen exchange isomer 1 (NHE1) inhibitor.BI-9627 partially reverses the effects of DMA with IC50 values of 6 and 31 nM in the intracellular pH recovery (pHi) and human platelet lysis assays.BI-9627 is often used as a negative control for BI-0054, which can be used for the study of ischemia-reperfusion injury in isolated hearts. BI-9627 is often used as a negative control for BI-0054 and can be used to study ischemia-reperfusion injury in isolated hearts.

MPO-IN-8, an orally active myeloperoxidase (MPO) inhibitor, effectively inhibits the production of hypochlorous acid in neutrophils and the release of extracellular traps (NETosis). In mice exhibiting gouty arthritis, it reduces swelling, decreases peroxidase activity, and lowers IL-1β levels.

CIB-1476, a caspase-1 inhibitor, effectively reduces joint swelling in mouse models of arthritis and demonstrates lasting anti-inflammatory effects. This compound achieves its benefits by blocking IL-1β production, NF-κB activation, and GSDMD-mediated pyroptosis, all of which are triggered by the NLRP3 inflammasome.

IL-17-IN-1 (26) is an orally active inhibitor of IL-17, demonstrating IC50 values of 0.013 μM for IL-17A and 0.004 μM for IL-6 release. It effectively alleviates knee joint swelling in a rat model of arthritis.

CHIKV-IN-5 (Compound 26) is an inhibitor of CHIKV with an EC90 value of 0.45 μM. It suppresses the replication of CHIKV in the later stages of the viral life cycle by blocking the translation of structural proteins. CHIKV-IN-5 demonstrates high stability in vitro within mouse microsomes. In infected mice, it alleviates footpad swelling and reduces the spread of the virus to other tissues.

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.

S-15176 is an inhibitor of the mitochondrial permeability transition pore (PTP). It effectively suppresses mitochondrial swelling induced by tert-butyl hydroperoxide, with an IC50 value of 45.7 μM. S-15176 prevents the opening of PTP, thus averting the dissipation of mitochondrial membrane potential and the oxidation of NAD(P)H, while enhancing mitochondrial calcium loading capacity. It holds potential for research into ischemia-reperfusion injury.

Dexamethasone acetate monohydrate is an adrenocortical steroid. It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, asthma, severe allergies, chronic obstructive lung disease, brain swelling, croup, and antibiotics

Naphazoline (Naphcon-a) is a sympathomimetic compound with marked alpha adrenergic activity. Naphazoline can be used as a vasoconstrictor with a rapid action in reducing swelling when applied to mucous membrane.

Zoniporide (CP-597396) is an NHE-1 inhibitor that inhibits the uptake of 22Na+ by fibroblasts expressing human NHE-1 in a concentration-dependent manner, inhibits platelet swelling, and can be used in the study of cardiovascular diseases.

BIX HCl is a sodium-hydrogen exchange type 1 inhibitor.

TC-AQP1-1 is a blocker of the aquaporin 1 channel identified by virtual screening and inhibits water flux through hAQP1 in Xenopus laevis oocyte swelling assays at low micromolar concentrations.

Berotralstat (BCX7353) is a second-generation, synthetic, and orally active plasma kallikrein inhibitor with low toxicity. It is highly specific and effectively used in the research of hereditary angioedema (HAE) attacks. Berotralstat functions by inhibiting the enzymatic activity of plasma kallikrein, which is responsible for the release of bradykinin. This blocking mechanism targets the major biologic peptide involved in the promotion of swelling and pain associated with HAE attacks[1][2].

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the production of reactive oxygen species (ROS) in, Hep3B human hepatocellular carcinoma cells. It does not induce cytotoxicity in RBL-2H3 mast cells at concentrations up to 100 μM. Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats. Exp.Brain.Res. 235 3033 PMID:28725925 |Kim et al (2017) Characterising the mode of action of extracellular Connexin43 channel mimetic peptides in an in vitro ischemia injury model. Biochem.Biophys.Acta. 1861 68 PMID:27816754 |Tonkin et al (2017) Attenuation of mechanical pain hypersensitivity by treatment with Peptide5, a connexin-43 mimetic peptide, involves inhibition of NLRP3 inflammasome in nerve-injured mice. Exp.Neurol. 300 1 PMID:29055716