Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR[1].
TLR7/8 agonist 7 (compound 10) is a TLR7/8 agonist. TLR7/8 agonist 7 activates a variety of immune cells and it can be used to synthesize immune stimulating antibody conjugate (ISAC) molecules. TLR7/8 agonist 7 can be used for the research of immunity[1].
JC-171 is a selective NLRP3 inflammasome inhibitor that inhibits LPS/ATP-induced IL-1β release from macrophages with IC50 of 8.45 uM; interferes with NLRP3/ASC interaction induced by LPS/ATP stimulation both in vtiro and in vivo; delays the progression and reduces the severity of experimental autoimmune encephalomyelitis (EAE).
25-Deacetylcucurbitacin A is a Cucurbitane-Type triterpenoid and has the potential to be an anti-cancer agent and JAK/STAT3 signaling pathway inhibitor[1].
D-Ribose(mixture of isomers) is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose(mixture of isomers) is active in protein glycation, induces NF-κB inflammation in a RAGE-dependent manner[1].
Erucin (ERU) is an isothiocyanate particularly abundant in arugula. Erucin shows anticancer, neuroprotective, and anti-inflammatory activities[1][2][3][4].
Cefditoren sodium (ME 1206) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren sodium has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren sodium can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections[1][2].
Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
Isoquercitrin is an effective antioxidant and an eosinophilic inflammation suppressor.
Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.IC50 value: Target: S1P1 agonistin vitro: Ponesimod activated S1P(1)-mediated signal transduction with high potency (EC(50) of 5.7 nM) and selectivity [1]. in vivo: Oral administration of ponesimod to rats led to a dose-dependent decrease of blood lymphocyte count. After discontinuation of dosing, blood lymphocyte count returned to baseline within 48 h. Ponesimod prevented edema formation, inflammatory cell accumulation, and cytokine release in the skin of mice with delayed-type hypersensitivity [1].
Mrgx2 antagonist-1 (example 1) is a potent Mrgx2 (Mas-related Gene X2) antagonist. Mrgx2 antagonist-1 can be used for the research of MrgX2-mediated diseases and disorders.
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
SB-747651A is a specific mitogen- and stress-activated kinase 1 (MSK1) inhibitor. SB-747651A can be used for the research of inflammation[1].
Trehalose 6-behenate is a Th1/Th17 skewing vaccine adjuvant.
Lck-IN-1 is a potent lymphocyte protein tyrosine kinase (Lck) inhibitor extracted from patent WO2007013673A1, example 48[1].
ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access[1][2].
Lepidiline B is a flavonolignan isolated from the roots of Brassicaceae Lepidium meyenii. Lepidiline B exhibits anti-inflammation activities in human cancer cell lines[1][2].
Nezulcitinib (TD-0903) is an inhaled and lung-selective pan-Janus kinase (JAK) inhibitor. Nezulcitinib can be used for the research of COVID-19 associated acute lung injury and impaired oxygenation[1][2].
Murabutide is a safe synthetic immunomodulator. Murabutide can reduce CD4 and CCR5 receptor expression and secrete high levels of beta-chemokines. Murabutide enhances nonspecific resistance against viral infections. Murabutide did not affect virus entry, reverse transcriptase activity or early proviral DNA formation in the cytoplasm of infected cells[1].
TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent[1][2][4].
3,4-Didehydroglabridin is a natural product that can be found in licorice. 3,4-Didehydroglabridin exhibits protective activities against carbon tetrachloride-induced HepG2 cells injury. 3,4-Didehydroglabridin has the potential for the research of liver injury[1][2].
COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase enzyme (15-LOX) inhibitor with IC50 values of 10.65, 0.075 and 2.98 μM against COX-1, COX-2 and 15-LOX, respectively. COX-2/15-LOX-IN-1 shows anti-inflammatory activity[1].
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis[1][2][3].
Nelumol A is a farnesoid X receptor (FXR) agonist[1].
ZK-90055 hydrochloride is a β2 adrenergic receptor agonist.
Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].
Quilizumab (Anti-Human NGcGM3 Recombinant Antibody) is a humanized IgG1κ monoclonal antibody. Quilizumab targets the M1-prime segment of membrane-expressed IgE, leading to depletion of IgE-switched and memory B cells. Quilizumab has the potantial for the asthma research[1].
L-Lysine hydrate is an essential amino acid. L-Lysine hydrate can be research for vascular calcification (VC) and acute pancreatitis[1][2].
Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'[1][2].