Inflammation/Immunology

Ceritinib (LDK378) dihydrochloride (Standard) is the analytical standard of Ceritinib dihydrochloride (HY-15656A). This product is intended for research and analytical applications. Ceritinib dihydrochloride is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib dihydrochloride also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency.

Lifitegrast-d₄ (SAR 1118-d₄) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC₅₀ of 2.98 nM. Lifitegrast can be used for researching dry eye disease.

M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases.

Boxidine is an orally active DHCR7 inhibitor. Boxidine inhibits DHCR7, blocks the conversion of 7-Dehydrocholesterol (HY-113279) to Cholesterol (HY-N0322), reduces serum cholesterol levels, causes accumulation of 7-dehydrocholesterol in serum and tissues, and inhibits sterol absorption. Boxidine exhibits antiproliferative and anticancer activities, with marginal activity against mouse tumors. Boxidine can be used in research related to diseases such as tumors and adrenal cancer.

AWD 12-281 is an orally active and highly selective phosphodiesterase 4 (PDE4) inhibitor (IC₅₀ = 9.7 nM). AWD 12-281 is used in the study of allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis.

β-Nicotinamide adenine dinucleotide reduced dipotassium is an orally effective reduced coenzyme. β-Nicotinamide adenine dinucleotide reduced dipotassium plays a role in regenerating electron donors during cellular energy metabolism, including glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle. β-Nicotinamide adenine dinucleotide reduced dipotassium regulates calcium homeostasis by promoting the opening of IP3-gated Ca²⁺ channels and inhibiting Ryanodine receptor, and affects mitochondrial function through direct interaction with VDAC. β-Nicotinamide adenine dinucleotide reduced dipotassium is used in cytoprotective studies related to cerebral ischemic injury, neurodegenerative diseases, aging, and signal transduction.

2-(Trifluoromethyl)cinnamic acid is a cinnamic acid derivative that inhibits the proton pump (H⁺/K⁺-ATPase), thereby reducing gastric acid secretion. 2-(Trifluoromethyl)cinnamic acid also improves delayed gastric emptying and can be used in research on gastric diseases such as acute gastritis and gastric ulcers.

Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.

FR183998 free base (Standard) is the analytical standard of FR183998 free base (HY-100302). This product is intended for research and analytical applications. FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.

NLRP3 modulator 7 (Compound 17B) TFA is a NLRP3 inflammasome modulator. NLRP3 modulator 7 TFA inhibits LPS (HY-D1056)-induced IL-1β release in fresh human whole blood. NLRP3 modulator 7 TFA can be used in studies related to NLRP3 inflammasome activation and innate immune signaling.

17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy.

Evrisiran is a prekallikrein synthesis reducer that has been studied for its potential use in hereditary angioedema.

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (Standard) (NSC95682 (Standard)) is the analytical standard of 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (HY-107371). This product is intended for research and analytical applications. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) (Compound 3-5) is a selective and potent IRE-1α inhibitor with an IC₅₀ value of 0.08 μM. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde can be used for research on diseases associated with the unfolded protein response (UPR), such as cancer and autoimmune diseases.

Genkwanin (Standard) is the analytical standard of Genkwanin. This product is intended for research and analytical applications. Genkwanin is a major non-glycosylated flavonoid with anti-flammatory activities.

9-Hydroxy-α-lapachone (α-Dihydrocaryopterone) is a natural phenol, exhibits potent inhibitory effects with an IC₅₀ of 4.64 µM on LPS-induced NO production in RAW 264.7 cells.

Cefazolin-¹³C₂,¹⁵N (sodium) is ¹³C and ¹⁵N labeled Cefazolin (sodium). Cefazolin sodium is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research. Cefazolin sodium has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD).

CGH 2466 dihydrochloride is an orally active adenosine A1, A2B and A3 receptor antagonist with the IC₅₀ values of 19 nM, 21 nM, and 80 nM respectively. CGH 2466 dihydrochloride inhibits p38 MAPK (IC₅₀ = 187~ 400 nM) and phosphodiesterase type 4D (IC₅₀ = 22 nM). CGH 2466 dihydrochloride displays potent anti-inflammatory effects both in vitro and in vivo, and can be used for research on asthma and chronic obstructive pulmonary disease (COPD).

DPA-714-d₁₀ is the deuterium labeled DPA-714 (HY-122607). DPA-714 is a high affinity translocator protein (TSPO) ligand (K_i=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. ¹⁸FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.

TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC₅₀ of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung.

Pegcetacoplan-¹³C₃,¹⁵N TFA is the ¹³C- and ¹⁵N-labeled Pegcetacoplan TFA. Pegcetacoplan is a pegylated complement C3/C3b inhibitor. Pegcetacoplan acts by specifically binding to and inhibiting C3 and C3b, thereby suppressing the complement cascade at its proximal stage. Pegcetacoplan is not a known inhibitor or inducer of CYP450 isoenzymes. Pegcetacoplan can be used for the research of complement-mediated diseases, including paroxysmal nocturnal hemoglobinuria (PNH) and age-related macular degeneration (AMD).