RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants[1].
WAY-PDA 641 is a potent and preferential PDE-IV inhibitor, with an IC50 of 0.42 μM for canine trachealis PDE-IV. WAY-PDA 641 induces respiratory muscle relaxation and bronchodilation[1].
ARN 077 enantiomer (19) is the less active enantiomer of ARN 077, with an IC50 of 3.53 μM for rat NAAA[1].
Longiferone B is a daucane sesquiterpene, that can be isolated from Boesenbergia longiflora rhizomes. Longiferone B shows anti-inflammatory activity against NO release with an IC50 of 21.0 μM. Longiferone B also suppresses the iNOS and COX-2 mRNA expression[1].
C3a receptor agonist 1 (compound benzeneacetamide) is a potent C3a receptor agonist. C3a receptor agonist 1 has the potential for the research of acute inflammation[1].
Protostemonine is an active alkaloid mainly isolated from the roots of Stemona sesslifolia, with anti-inflammatory activity. Protostemonine has anti-inflammatory effects on asthma and gram-negative bacteria-induced acute lung injury[1][2].
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors[1].
Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM[1].
Hydralazine is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel. Hydralazine has antioxidant activity, as well as inhibits reactive oxygen species (ROS) release and O2·- generation with an IC50 value of 9.53 mM and 1.19 mM, respectively[1][2].
Guaifenesin-d5 (Guaiacol glyceryl ether-d5) is the deuterium labeled Guaifenesin. Guaifenesin (Guaiacol glyceryl ether), a constituent of guaiac resin from the wood of Guajacum officinale Linné, is an expectorant. Guaifenesin can alleviate cough discomfortby increasing sputum volume and decreasing its viscosity, thereby promoting effective cough. Guaifenesin also has narcotic effect[1][2].
Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
Influenza Matrix Protein (61-72) is a peptide fragment derived from matrix protein of influenza viruses, corresponds to amino acids 61-72. Influenza Matrix Protein (61-72) is a specific epitope which can induce CD4+ T-cell response[1].
Tr-PEG3-OH is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease[1].
Neoisoastilbin possesses antioxidant, anti-hyperuricemic and anti-Inflammatory activities[1].
Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab. Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL)[1].
Me-triacetyl-β-D-glucopyranuronate-Ph-ald-NO2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake[1].
Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20+ non-Hodgkin lymphomas (NHL)[1][2].
FKKSFKL-NH2 is a protein kinase C-selective peptide. FKKSFKL-NH2 can be used for the research of various biochemical[1].
AR-C141990 is a lactate transporters inhibitor.
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM[1].
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].
Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity[1][2].
AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease[1].
Misoprostol acid D5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent[1].
Ipsalazide is a novel sulfasalazine analog designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract.
Gemcabene calcium (PD-72953 calcium), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity[1][2][3].