Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties[1][2].
Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1][2].
Ocarocoxib, a potent COX-2 (cyclooxygenase-2) inhibitor, is a non-steroidal anti-inflammatory for veterinary use[1].
Ibuprofen Impurity K is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1].
Histamine H4 receptor antagonist-1 is an antagonist of histamine H4 receptor extracted from patent WO2010108059A1 compound 60[1].
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity[1].
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research[1][2].
4-Methylhistamine (dihydrochloride) is the potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine (dihydrochloride) has the potential for the research of immune-related diseases such as cancer and autoimmune disorders[1].
Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM)[1][2][3].
GNE-2256 (GNE2256) is a potent, selective inhibitor of IRAK4 with biochemical Ki of 1.4 nM.GNE-2256 displays high selectivity in the CEREP panel with off-targets with >50% inhibition are TACR1, HTR2B and ACHE.GNE-2256 is potent in the NanoBRET assay (IC50 = 3.3 nM), the IL-6 human whole blood assay (IC50=190 nM) and the IFNα human whole blood assay (IC50=290 nM).
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Bavisant (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. IC50 Value: Target: H3 receptorin vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1].in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/day groups with placebo based on a step-down closed testing procedure were not performed [2].Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2
CY-09 is an NLRP3 inhibitor.
NLRP3-IN-11 is a NLR family pyrin domain containing 3 (NLRP3) proteins inhibitor. NLRP3-IN-11 has biological activity for NLRP3 with an IC50 value of ＜0.3 μM. NLRP3-IN-11 can be used for the researh of inflammatory and degenerative diseases including NASH, atherosclerosis and other cardiovascular diseases, Alzheimer's disease, Parkinson's disease, diabetes, gout, and numerous other autoinflammatory diseases[1].
MK886 is a 5-lipoxygenase-activating protein inhibitor and a leukotriene biosynthesis inhibitor (IC50=2.5 nM).
Piroxicam cinnamate (Cinnoxicam) is a cyclooxygenase (COX) inhibitor, with anti-inflammatory activity. Piroxicam cinnamate is stable under gastric conditions, can be used for inflammatory-degenerative osteoarticular diseases, rheumatic disorders, and varicocele (VC) associated oligoasthenospermia research[1][2][4].
Keliximab (SB-210396) is a chimeric human/macaque IgG1 anti-CD4 monoclonal antibody with a Ki value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research[1][2].
Cetrelimab (JNJ 63723283; JNJ 3283) is a humanized IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo[1].
Guretolimod is a Toll-like receptor 7 (TLR7) agonist[1].
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].
AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range[1]. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis[3].
Pemirolast Potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.Target: Histamine H1 ReceptorPemirolast potassium (BMY 26517) is a new oral, nonbronchodilator antiallergy medication that is being evaluated for the therapy of asthma [1]. Pemirolast potassium (BMY 26517) inhibits chemical mediator release from tissue mast cells and is also shown to inhibit the release of peptides including substance P, Pemirolast potassium (BMY 26517) reduces kaolin intake by inhibition of substance P release in rats [2]. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats [3]. Pemirolast potassium is used for the treatment of allergic conjunctivitis and prophylaxis for pulmonary hypersensitivity reactions to drugs such as paclitaxel [4].
Shanciol B, isolated from the ethyl acetate extract of the air-dried whole plant of Pholidota imbricate Hook, inhibits nitric oxide (NO) production and 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity[1]. Shanciol B is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with anti-inflammatory activity[2].
Efmarodocokin alfa is a fusion protein of human IL-22 and the IgG4 crystallizable fragment. Efmarodocokin alfa activates IL-22 signaling. Efmarodocokin alfa can be used for the research of severe COVID-19 pneumonia[1].
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
ODN 21595 is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 reduces the expression of CD86 and HLA-DR. ODN 21595 has the potential for the research of systemic lupus erythematosus (SLE)[1].
Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.
Epibetulinic acid, isolated from the root bark of Maytenus cuzcoina and the leaves of Maytenus chiapensis, exhibits potent inhibitory effects on NO and prostaglandin E2 (PGE2) production in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin with IC50s of 0.7 and 0.6 μM, respectively. Anti-inflammatory activity[1].
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM[1][2][3].
TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.