S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.
Gamma-glutamylcysteine (γ-Glutamylcysteine), a dipeptide containing cysteine and glutamic acid, is a precursor to glutathione (GSH). Gamma-glutamylcysteine is a cofactor for glutathione peroxidase (GPx) to increase GSH levels[1].
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].
Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR[1][2][3].
Sphinganine 1-phosphate-d7 is deuterium labeled Sphinganine 1-phosphate. Sphinganine 1-phosphate (D-erythro-Dihydrosphingosine 1-phosphate) is a polar sphingolipid metabolite that regulates cell migration, differentiation, survival and complex physiologic
Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.Target: AntifungalSertaconazole nitrate reduces the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation in a dose-dependent fashion. Sertaconazole nitrate is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL [1]. Sertaconazole nitrate inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. Sertaconazole nitrate binds directly to nonsterol lipids in the membrane, which interferes with the regulation of the permeability of fungal cell membranes, thus induces fungal cell death [2].The mean ear weight of Tetradecanoyl phorbol acetate (TPA)-challenged murine treated with sertaconazole nitrate (1%) is 7.23 mg compared with 14.7 mg for controls, indicating a statistically significant reduction in irritant dermatitis. Sertaconazole nitrate 1% elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with sertaconazole nitrate 1% significantly inhibits contact hypersensitivity and decreases the content of the pro-inflammatory cytokines TNFα, IL-2, and IFNγ in oxazolone exposed murine skin [1]. Clinical trials with sertaconazole nitrate cream 2% show efficacy in the treatment of superficial cutaneous fungal infections [2]. Sertaconazole reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks sertaconazole from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema [3].
NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research[1].
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B[1].
6-[(4-Oxo-1,2,3-benzotriazin-3-yl)methylthio]hexanoic acid (MBH) is a hapten with a carboxyl group at the end of its spacer arm, suitable for reacting with free amine groups of proteins. 6-[(4-Oxo-1,2,3-benzotriazin-3-yl)methylthio]hexanoic acid can be combined with carrier proteins and used in antigen design[1].
Fasciculic acid A is a steroid that can be isolated from Hypholoma lateritium. Fasciculic acid B has antiinflammatory and calmodulin antagonistic activity[1].
Pinostrobin is a flavonoid can be found in many plants, and has anti-oxidant, anti-inflammatory, anti-cancer and neuroprotective properties. Pinostrobin is a potent PCSK9 inhibitor and inhibits the catalytic activity of PCSK9. Pinostrobin is a promising agent for cholesterol regulation and lipid management[1].
Apterin is a natural compound with anti-inflammatory activity. Apterin shows significantly inhibitory activity on NO production in RAW264.7 cells with an IC50 value of 41.8 μM[1].
Forskolin is a potent adenylate cyclase activator, with IC50 and EC50 of 41 nM and 0.5 μM for type I adenylyl cyclase, respectively.
TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα (KD = 6.8 nM).
Cecropin D is an antimicrobial peptide with a MIC of 4.55 μg/mL. Cecropin D is effective against both Gram-negative and Gram-positive bacteria. Cecropin D has antiviral, antifungal, antitumor, and immunomodulatory[1][2].
Azadirachtin B is an limonoid isolated from seed kernels of Azadirachta indica. Azadirachtin B increases alkaline phosphatase (ALP) activity and stimulates osteoblast differentiation. Azadirachtin B is active against the Epstein-Barr virus early antigen (EBV-EA). Azadirachtin B has insecticidal, nematocidal, anticancer, anti-inflammatory, antiviral and osteogenic properties[1][2][3].
Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties[1][2].
6-N-Phthalimidoy hexanoic acid (compound FH) is a hapten with a carboxyl group at the end of its spacer arm, suitable for reacting with free amine groups of proteins. 6-N-Phthalimidoy hexanoic acid can be combined with carrier proteins and used in antigen design[1].
ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, which can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD)[1].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Ibudilast-d3 (KC-404-d3) is the deuterium labeled Ibudilast. Ibudilast (KC-404) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[1][2].
PKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system[1].
Oleanolic acid derivative 1 is an oleanolic acid derivative, which is a novel triterpenoid-steroid hybrid molecule.
Setrusumab (BPS 804) is a fully humanized monoclonal antibody targets sclerostin. Setrusumab efftively improves bone strength. Setrusumab can be used for the resesrch of Osteogenesis Imperfecta (OI) and cancer[1].
Rosiglitazone maleate is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
Isocarlinoside, a di-C-glycosylflavone from Lespedeza capitate[1].
Lotamilast is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells[1][2].
Disialyllacto-N-tetraose is a human milk oligosaccharide that prevents necrotising enterocolitis in neonatal rats[1].
Z-Ala-Ala-Asp-CMK (Z-AAD-CMK) is a selective granzyme B inhibitor[1].