Ebastine-d5 (LAS-W 090-d5) is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1][2].
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis.
Clopirac is a potent and orally active inhibitor of prostaglandin synthetase. Clopirac is an anti-inflammatory agent[1].
Balsalazide-d4 is deuterium labeled Balsalazide. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
PD-1/PD-L1-IN-33 (Compound N11) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-33 inhibits PD-1 and PD-L1 interaction with an IC50: 6.3 nM. PD-1/PD-L1-IN-33 promotes T-cell proliferation, activation, and infiltration into tumor spheres. PD-1/PD-L1-IN-33 has immunomodulatory and anticancer activity[1].
Astemizole, a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has anticholinergic and antipruritic effects[1][2].
3-Bromo-7-nitroindazole is a more potent and selective inhibitor of neuronal nitric oxide synthase (nNOS) than eNOS or inducible nitric oxide synthase (iNOS). 3-Bromo-7-nitroindazole affects the intercellular messenger nitric oxide (NO) synthesis throughout the body and brain[1].
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects[1].
Olopatadine-d3 hydrochloride (ALO4943A-d3) is the deuterium labeled Olopatadine hydrochloride. Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis[1][2].
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity[1][2][3].
Opucolimab is an anti-PD-L1 recombinant human monoclonal antibody. Opucolimab can be used to synthesis antibody drug conjugates. Opucolimab can be used for the research of advanced solid tumors[1].
Izokibep (ABY-035) is a selective and antibody mimetic interleukin 17A (IL-17A) inhibitor with high potency and long half-life. Izokibep can be used for the research of ankylosing spondylitis, atherosclerosis and skin disease[1].
ODN 1668, a class B CpG ODN (oligodeoxynucleotide), is a TLR-9 agonist. ODN 1668 is an immunostimulatory sequence and can be used as vaccine adjuvant. Sequence: 5'-tccatgacgttcctgatgct-3’[1][2].
Depemokimab (GSK-3511294) is a long-acting anti-IL-15 monoclonal antibody. Depemokimab can be used for research of asthma[1][2].
BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer[1].
Fezakinumab is an interleukin-22 (IL-22) monoclonal antibody. Fezakinumab can be used for the research of inflammatory disease, such as psoriasis and rheumatoid arthritis[1].
Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research[1][2][3].
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
Factor B-IN-2 (Example 1 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.5 μM. Factor B-IN-2 can be used for the research of diseases related to inflammation and immunity[1].
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues[1].
Atractylochromene is a potent dual inhibitor of 5-LOX/COX-1 with IC50s of 0.6 and 3.3 μM, respectively[1].
Eltrombopag methyl ester is a derivative of Eltrombopag, which is a thrombopoietin (Tpo) receptor agonist, which can promote platelet production and is used in research related to specific types of thrombocytopenia[1].
GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines[1][2].
Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock[1][2].
TLR8 agonist 2 is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 shows less active against human TLR7 (EC50 of 33.33 μM)[1].
Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].
CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration[1].
PPM-18 (NSC 73233), a potent anti-inflammatory agent, inhibits nitric oxide synthase expression. PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter[1]. PPM-18, an analog of Vitamin K, induces autophagy and apoptosis in bladder cancer cells through ROS and AMPK signaling pathways[2].
Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders[1].