7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer with an IC50 value of 6.9 nM against CXCR4-specific antagonist peptide, TN14003. CXCR4 probe 1 has potential to be used as CXCR4-specific imaging probe to diagnose and monitor the prognosis of inflammatory diseases, CXCR4-positive tumors, and metastatic cancers[1].
Toralizumab (IDEC-131) is a humanized monoclonal antibody (mAb) against CD40L (CD154) comprised of human gamma 1 heavy chains and human kappa light chains. Toralizumab binds specifically to human CD40L on T cells, thereby preventing CD40 signaling. Toralizumab, a immunosuppressive drug, has the potential for active systemic lupus erythematosus (SLE) research[1][2].
CD80-IN-3, a potent CD80 inhibitor, inhibits CD80/CD28 interaction with an EC50 of 630 nM and a Kd of 125 nM.
Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, extracted from patent WO 2019026065A2 [1].
CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
Fentiazac, alkanoic acid derivative, is an orally active non-steroidal anti-inflammatory agent, with analgesic, antipyretic and platelet anti-aggregation activity. Fentiazac can be used to research inflammatory diseases such as rheumatoid arthritis, osteoarthritis and tendinitis[1][2][3].
14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide that can be isolated from A. paniculata. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively[1][2].
Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV[1].
Diprovocim is a potent Toll-like receptor TLR1/TLR2 agonist that induces dose-dependent TNF production with EC50 of 110 pM in human THP-1 cells and 1.3 nM in primary mouse peritoneal macrophages; induces TNF production in bone marrow-derived dendritic cells (BMDC) with EC50 of 6.7 nM, also induces IL-6 production by mouse BMDC; induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages, activates conventional TLR1/TLR2 signaling, including MAPK and canonical NF-κB signaling; synergizes with anti-PD-L1 to eliminate melanoma in mice.
Isoflupredone belongs to the class of corticosteroids and exerts its effect by binding to glucocorticoid and mineralocorticoid receptors of animals, such as horses. Isoflupredone can be used in wide range of conditions, such as infection and inflammatory diseases[1].
Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
P2X3 antagonist 36 is a P2X3 antagonist extracted from patent WO2019081343A1 compound 156[1].
Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis[1][2].
Briakinumab (ABT-874) is a fully human anti-IL-12/23p40 monoclonal antibody. Briakinumab targets and neutralizes IL-12 and IL-23. Briakinumab can be used for the research of rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis[1].
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury[1][2][3].
A novel Glucocorticoid receptor modulator.
Avizakimab (BOS161721) is a humanized IgG1 monoclonal antibody that targets interleukin-21[1].
PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
KIRA-7 is a small molecule inhibitor of IRE1α kinase/Rnase with IC50 of 0.11/0.22 uM, allosterically inhibits IRE1α RNase activity; reverses bleomycin-induced fibrosis when given 2 weeks after bleomycin exposure in vivo.
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs)[1].
Pipebuzone (LD 4644) is an anti-inflammatory, antipyretic and analgesic agent. Pipebuzone plays an important raol in rheumatic diseases[1].
LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.
Magnesium silicate (Activated magnesium silicate) is a compound of magnesium oxide (MgO) and silicon dioxide (SiO2). Magnesium silicate is used in antiacid and antiulcer preparation, and as a deodorizer, decolorizer and antifungal[1].
COX/5-LOX-IN-1 (compound 6b) is a potent and dual inhibitor of COX/5-LOX with IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively. COX/5-LOX-IN-1 has the potential for the research of inflammation diseases[1].
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect[1].
Lonazolac is a non-steroidal antirheumatic agent. Anti-inflammatory effects [1].
Antitumor agent-56 (Compound 33) is a triptolide derivative with antitumor, anti-inflammatory and NO release activities. Antitumor agent-56 significantly inhibits the growth of melanoma. Antitumor agent-56 is orally active[1].