Lansoprazole sodium(AG-1749) is a proton pump inhibitor which prevents the stomach from producing acid.Target: Proton PumpLansoprazole (sodium) is sodium salt form of lansoprazole, lansoprazole, a substituted benzimidizole proton pump inhibitor, on pharmacokinetics and metabolism of theophylline has been studied in healthy adults given oral lansoprazole 30 mg once daily for 11 days. On Days 4 and 11 of 300 mg aminophylline was simultaneously administered orally and blood samples for theophylline analysis were taken over 24 h [1]. Patients in the lansoprazole group were significantly less likely to have a recurrence of ulcer complications than patients in the placebo group (P=0.008). There was no significant difference in mortality between the two groups [2]. lansoprazole (AG-1749) and omeprazole, were found to have significant activities against this organism. The activity of lansoprazole was comparable to that of bismuth citrate, with MICs ranging from 3.13 to 12.5 micrograms/ml, and fourfold more potent than that of omeprazole [3]. Clinical indications: Duodenal ulcer; Esophagitis; Gastroesophageal reflux; Gastrointestinal disease; Helicobacter pylori infection; Peptic ulcer; Stomach ulcer; Ulcer; Zollinger-Ellison syndromeFDA Approved Date: May 10, 1995Toxicity: Symptoms of overdose include abdominal pain, nausea and diarrhea.
Isophysalin G is a steroid that inhibits NO production induced by Lipopolysaccharides (HY-D1056) in macrophages with an IC50 of 64.01 μM[1].
Dnp-GPLGMRGL-NH2 is a peptide substrate for matrix metalloproteinase-13 (MMP-13) with a kcat/Km value of 4,200,000 M-1s-1.
Hepatitis b virus pre-s region (120-145) is a preS2 peptide that inhibits the binding of single-chain Fv fragment (scFv) or IgG to r-HBsAg[1].
Fulvic Acid is a natural healthy product, which comes from humic substances produced by microorganisms in soil. Fulvic Acid can modulate the immune system, influence the oxidative state of cells, and improve gastrointestinal function. Fulvic Acid has the potential for the treatment of chronic inflammatory diseases, including diabetes[1].
AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM; shows excellent selectivity over PAR1 and PAR4 (>50 uM).
AA 2379 is an orally active antirheumatic agent. AA 2379 has antiinflammatory, antipyretic activities and reduces pain sensation[1].
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM[1].
Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].
Cotransin is a Sec61 translocation inhibitor that acts in a signal-sequence-discriminatory manner to prevent the stable insertion of select nascent chains into the Sec61 translocation channel. Cotransin selectively inhibits the expression of VCAM-1 and p-selectin proteins by inhibiting their co-translational translocation across endoplasmic reticulum (ER) membranes (IC50=0.5-5 µM). Cotransin has potential for studying inflammation and immunity[1][2].
α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER),α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects[1].
Oxindole (Indolin-2-one) is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].
Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis [1][2].
Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis[1].
β-Interleukin II (44-56) is a 44-56 fragment of beta-interleukin II polypeptide. Interleukin family are a group of cytokines associated with immune system, mainly expressed by leukocytes[1].
Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus (Fisch.) Bunge[1].Astramembrangenin is orally safe and has broad Extensive pharmacological effects, including telomerase activation, telomere elongation, anti-inflammatory and anti-oxidative properties[2].Astramembrangenin has antiaging properties, CAG stimulates telomerase activity in human neonatal keratinocytes and rat neuronal cells, and induces CREB activation followed by tert and bcl2 expression. Cycloastragenol (CAG) may have a novel therapeutic role in depression[2].
M4284 (M-4284) is a high-affinity biphenyl mannoside FimH inhibitor with HAI of 16 nM in hemagglutination assay; reduces intestinal colonization of genetically diverse UPEC isolates, while simultaneously treating UTI, without notably disrupting the structural configuration of the gut microbiota; reduces UTI89 levels in the gut and urinary tracts of mice.
N-(β-ketocaproyl)-L-Homoserine lactone is a component of quorum regulatory sensing[1].
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties[1][2]. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders[1]. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages[2].
Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
Glafenine is a non-steroidal anti-inflammatory drug (NSAID), is a non-narcotic analgesic agent, widely used for the treatment of pains of various origins.
Lumiracoxib-d6 (COX-189-d6) is the deuterium labeled Lumiracoxib. Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a Ki value of 0.06 μM[1]. Lumiracoxib acts as a nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research[1][2].
Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].
EGTA tetrasodium is a specific calcium ion chelator. EGTA tetrasodium has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca2+ over Mg2+ (Mg2+ Kd 1-10 mM). EGTA tetrasodium significantly inhibits the substrate adherence capacity of inflammatory macrophages[1][2].
GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively[1].
Quinaldopeptin, a quinomycin antibiotic isolated from the culture of Streptoverticillium album strain, is highly active against Gram-positive bacteria and anaerobes and strongly cytotoxic against cultured B16 melanoma cells[1].
Muromonab is a monoclonal antibody targeting the CD3 receptor. Muromonab can block all cytotoxic T cell function. Muromonab also as an immunosuppressant agent given to reduce acute solid organ transplant rejection[1].
A novel potent, selective Sirt2 inhibitor with IC50 of 0.118 uM; displays no inhibitory activity against Sirt1 and Sirt 3 (IC50>100 uM).