Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment[1].
Atrosab is a humanized IgG1 antagonistic anti-TNFR1 antibody. Atrosab inhibits TNF-mediated apoptosis induction and IL-6 and IL-8 production. Atrosab can be used for research of inflammatory disease[1].
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively[1].
IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM[1].
Lanadelumab (SHP643) is a humanized IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema[1][2].
Bayogenin 3-O-β-D-glucopyranoside, a triterpenoid saponin isolated from Polygala japonica, possesses anti-inflammatory activities[1].
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells[1].
5-OH-HxMF is a hydroxylated polymethoxyflavone that has anti-inflammatory, anticancer, neurotrophic and neuroprotective activities[1][2][3].
(-)-Corypalmine (Discretinine), an alkaloid that could be isolated from the stem of Guatteriopsis friesiana, possesses antimicrobial activity[1].
L 012 sodium salt a luminol-based chemiluminescent (CL) probe, is widely used in vitro and in vivo to detect NADPH oxidase (Nox)-derived superoxide (O2•−) and identify Nox inhibitors[1].
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research[1][2][3].
V-116517 is a novel potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM; shows high selectivity for TRPV1 over TRPV3 and TRPV4 (>10 uM) in a panel of 66 ion channels, receptors, transporters; dose-dependently reverses thermal hyperalgesia with ED50 of 2 mg/kg (p.o.) in acute inflammatory CFA model; shows excellent aqueous solubility, metabolic stability, oral bioavailability in multiple species, and excellent efficacy in a variety of animal pain models. Pain Phase 2 Clinical
Sar-[D-Phe8]-des-Arg9-Bradykinin is a agonist of B1 receptor. Sar-[D-Phe8]-des-Arg9-Bradykinin selectively amplifies the contractile response when incubation with human recombinant interleukin-1 β (IL-1 β) in rabbit aortic rings[1].
Platyconic Acid A is an active component of changkil saponins from platycodon grandiflorum and can be used for the research of reducing airway inflammation[1].
Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 µM and 7.39 µM, respectively[1]. Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity[2].
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC50 of 163 nM[1].
Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows anti-inflammatory activity in models of murine colitis[1].
L 601920-0 is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
Benzoylgomisin O isolated from Schisandra rubriflora, has inhibitory activity against 15-LOX, COX-1 and COX-2 enzymes and anti-inflammatory activity[1].
Fasinumab (Anti-Human NGF) is a human IgG1k monoclonal antibody to nerve growth factor (NGF). Fasinumab can be used in acute sciatica and knee osteoarthritis (OA) studies[1].
Ayanin is a bioflavonoid isolated from Croton schiedeanus Schlecht. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al[1].
Kebuzone is a non-steroidal anti-inflammatory substance that may be studied in inflammatory diseases such as thrombophlebitis and rheumatoid arthritis[1].
N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
Tomentin is a compound isolated from Sphaeralcea angustifolia. Tomentin inhibits the formation of λ-carrageenan footpad edema at 58 %. Tomentin inhibits the phorbol ester-induced auricular edema formation by 57 %[1].
ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.
Antibacterial agent 129, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis and B. subtilis with MICs of 31.25 μM and 31.5 μM and . Antibacterial agent 129 shows good antifungal activity against A. niger with a MIC of 31.25 μM. Antibacterial agent 129 shows excellent antimycobacterial activity with MIC 57.73 μM for M. tuberculosis H37Rv[1].
Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure[1].
Taurodeoxycholate-d6 (sodium salt) is the deuterium labeled Taurodeoxycholate sodium salt[1]. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[2]. [2][3].
(E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC50s of 1.12 and 0.83 μM, respectively[1].