L-Arginine-1,2-13C2 ((S)-(+)-Arginine-1,2-13C2) hydrochloride is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Diphenylpyraline Hcl is a first-generation antihistamine with anticholinergic effects, acts as a dopamine reuptake inhibitor, shows to be useful in the treatment of Parkinsonism.
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research[1][2].
C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides[1]. C6 L-threo Ceramide significantly inhibits IL-4 production in T cells. Anti-allergic agents[2].
Dimethoxycurcumin is a derivative of curcumin that has anti-inflammatory and antioxidant activities[1][2].
YKL-05-099 is a salt-inducible kinase (SIK) probe; inhibits SIK2 with an IC50 of 40 nM.
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-bindingoligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX)[1].
NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitory activity against NO production, with an IC50 of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research[1].
Afasevikumab (RG 7624; RO 5553110; NI-1401) is a fully human monoclonal IgG1κ antibody neutralizing both IL-17A and IL-17F. Afasevikumab has anti-inflammatory activities[1].
Cetirizine D4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
WH-4-025 is a Salt-inducible kinase (SIK) inhibitor (WO2016023014 A2)[1].
Oxelumab (R 4930) is a human monoclonal antibody against the OX40 ligand (OX40L). Oxelumab can be used for the research of asthma[1].
Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
STING agonist-34 (Compound 12L) is a potent STING agonist with an IC50 value of 1.15 μM and an EC50 of 0.38 μM in THP1 cells. STING agonist-34 could be used in cancer research[1].
Alismol is a natural sesquiterpene. Alismol shows promising inhibitory effects on INF-γ-induced nitric oxide production in murine macrophage RAW264.7 cells[1].
ML339 is a potent and selective CXCR6 (IC50 of 140 nM) antagonist that is selective (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ). ML339 holds potential to advance the field of prostate cancer research[1].
Resiquimod-d5 (R848-d5) is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α[1][2].
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
Famotidine-13C,d3 is the 13C- and deuterium labeled. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
COX-2/5-LOX-IN-3 (compound 5b) is a potent and dual COX-2/5-LOX inhibitor with IC50 values of 45.73, 5.45 and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. COX-2/5-LOX-IN-3 has the potential for the research of inflammation diseases[1].
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM[1].
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research[1].
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50 of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
Bryonolic acid is an active triterpenoid compound with immunomodulatory, anti-inflammatory, antioxidant and anticancer activities[1][2][3].
STING agonist-26 (CF508) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive drug.
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, inhibits migration and induces cytotoxicity in CXCR4-expressing ovarian cancer cells[1][2].
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon[1].
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1[1].
Ro26-4550 is a low micromolar antagonist of IL-2/IL-2Rα binding with an IC50 value of 3 μM[1].