Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively, and possesses lipid-lowering effect.
MIF-IN-3 is a migration inhibitory factor (MIF) inhibitor extracted from patent WO2021258272A1 compound 31. MIF-IN-3 can be used for the research of immune inflammation-related diseases[1].
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF)[1].
Monoethylglycinexylidide is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver[1].
Hydroxyzine pamoate is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 ug/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].
COX-2-IN-1 is potent and slective COX-2 inhibitor with an IC50 of 3.9 μM.
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant in combination with a HER2 inhibitor, works on ER+/HER2+ cancer[1][2].
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.
Oxazolone is a haptenizing agent that induces acute or chronic inflammation of the large intestine and is used to construct models of colitis. Oxazolone can cause Th1/Th2-dependent colitis with weight loss and diarrhea. Oxazolone-induced inflammation can be mitigated by neutralizing anti-IL-4 or anti-TNF-α antibodies or decoy IL-13R2-α-FC proteins[1].
VRT-532 (CFpot-532) is a potent is a potent CFTR modulator. VRT-532 enhances channel activity in G551D-CFTR and intrinsic ATPase activity of G551D-CFTR. VRT-532 has the potential for the research of cystic fibrosis[1][2].
Sodium zirconium cyclosilicate is an orally administered, non-absorbed, novel, inorganic microporous zirconium silicate compound, is a highly selective cation exchanger that selectively removes excess K+ in vivo. Sodium zirconium cyclosilicate can be used in research of chronic kidney disease (CKD)[1][2].
Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine is used for the study of rheumatoid arthritis (RA)[3].
Ristomycin sulfate is a glycopeptide antibiotic isolated from Nocardia lurida[1].
Desmethyl Celecoxib (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%[1].
Rhamnazin is an orally active inhibitor of VEGFR2 signaling with an IC50 of 4.68 μM against VEGFR2 kinase. Rhamnazin shows potent antiangiogenic activity and antitumor efficacy[1]. Rhamnazin shows antioxidant and anti-inflammatory properties[2].
Methopterin inhibits osteoclasts proliferation. Methopterin inhibits the activation and bone resorption function of osteoclasts, and induced osteoclasts apoptosis[1].
Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects[1][2][3][4].
Schineolignin B is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities[1].
Cefotaxime, a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria[1][2][3][4].
Tilomisole (Wy 18251) is a benzimidazothiazole experimental drug with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation[1][2].
SR-31747 is a new sigma ligand with immunosuppressive properties.
L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH)[1][2].
AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
Ac-Trp-Glu-His-Asp-Aldehyde is a potent and selective caspase-1 inhibitor with a Ki value of 56 pM[1][2].
Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases[1][2].
SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
Drotrecogin alfa activated (DrotAA) is recombinant human activated protein C (APC). Drotrecogin alfa activated prevents smoke-induced increases in pulmonary microvascular permeability and proinflammatory cytokine IL-1β in rats. Drotrecogin alfa activated inhibits coagulation and inflammation and promotes fibrinolysis. Drotrecogin alfa activated can be used for severe sepsis reaearch[1][2].
Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment[1].
(3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities[1].
cFMS-IN-2 is a FMS kinase inhibitor with an IC50 of 0.024 μM.