Bevenopran is a peripheral μ-opioid receptor antagonist.
Clocortolone pivalate is a synthetic glucocorticoid corticosteroid and corticosteroid ester. Clocortolone pivalate is indicated for seborrheic dermatitis, contact dermatitis, atopic dermatitis and psoriasis[1].
PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity[1].
Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases[1][2].
TMDJ-035 is a selective RyR2 inhibitor. TMDJ-035 suppresses abnormal Ca2+ waves and transients in isolated cardiomyocytes from RyR2-mutated mice. TMDJ-035is a tool for studying the mechanism and dynamics of RyR2 channel gating[1].
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10[1][2].
FBBBE is used to detect the production of H2O2 by cells. FBBBE can be triggered by intracellular H2O2 and converted to fluorescein, resulting in an increase in intracellular fluorescence (Ex=4480 nm, Em=512 nm)[1].
BMS-582949 hydrochloride is a novel highly selective p38α MAPK inhibitor, inhibits p38α with IC50 of 13 nM. IC50 value: 13 nM[1]Target: p38αin vitro: BMS-582949 does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 with IC50values >40 μM. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. BMS-582949 is also 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective over Raf[1].BMS-582949 is a novel highly selective p38α MAPK inhibitor [2]. in vivo: The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And, at an oral dose of 10 mg/kg, the mouse AUC0?8 h for BMS-582949 is 75.5 μM·h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1].
SRTCX1003 is an orally active SIRT1 activator. SRTCX1003 suppresses inflammatory responses[1].
Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM.
PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.
Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome[1][2].
GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma[1].
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release[1][2].
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].
RDN2150 (Compound 25) is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 covalently binds to the C346 residue of ZAP-70. RDN2150 inhibits the expression of CD25 and CD69, and inhibits CD4+ T cell activation. RDN2150 can be used for research of psoriasis[1].
Cornoside is a phenolic glycoside and has inhibitory effect on rat lens aldose reductase (AR) with an IC50 of 150 μM[1].
Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia[1].
Pam3-Cys-Ala-Gly, a synthetic bacterial lipopeptide, is a potent macrophage and B cell activator[1].
Enazadrem is a 5-lipoxygenase inhibitor with antiinflammatory activities.
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate[1]. Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products[2]. A systemic acquired resistance (SAR) signal in tobacco[3]. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor[5].
Orilanolimab (SYNT001) is a humanized, de-immunized and FcRn-blocking monoclonal antibody. Orilanolimab blocks the interaction between FcRn and the Fc portion of IgG molecules. Orilanolimab impedes IgG IC activation of the FcRn-mediated adaptive immune function. And Orilanolimab disrupts the associated pathways related to IgG homeostasis and innate and adaptive immunity[1][2].
Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation[1].
diABZI STING agonist-1 (Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease[1][2][3][4].
Alpha-cyperone is associated with the down-regulation of COX-2,IL-6,Nck-2,Cdc42 and Rac1, resulting in reduction of inflammation. which would be highly beneficial for treatment of inflammatory diseases such as AD.In vitro: The anti-inflammatory activity of alpha-cyperone is associated with the down-regulation of COX-2 and IL-6 via the negative regulation of the NFκB pathway in LPS-stimulated RAW 264.7 cells.[1]Alpha-Cyperone binds and interacts with tubulin and is capable of distinctly destabilizing microtubule polymerization. The effect of this interaction could result in reduction of inflammation which would be highly beneficial for treatment of inflammatory diseases such as AD. One microliter of alpha-Cyperone was dissolved in DMSO (1:1 v/v) and it was further diluted in double distilled water (ddH2O) to a final volume of 20 microliter. [2]
MC-4R Agonist 2 hydrochloride (Example 1) is a MC4R agonist. MC-4R Agonist 2 hydrochloride can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction[1].
Dexamethasone 9,11-epoxide, a compound extracted from patent CN 106520896 A and RU 2532902 C1, is an intermediate in the preparation of dexamethasone.
Corymbosin is a glucoside. Corymbosin can be isolated from the aerial parts of Ballota glandulosissima. Corymbosin also has antifungal flavonoid activity[1][2].
Superoxide dismutase (SOD) is the only antioxidant enzyme that scavenges the superoxide anion by converting this free radical to oxygen and hydrogen peroxide, thus preventing peroxynitrite production and further damage. Superoxide dismutase is extensively researched and used in anti-inflammatory, antitumor, radiation protection, and antisenility applications[1].