Vilanterol-d4 (trifenatate) is deuterium labeled Vilanterol (trifenatate). Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor (β2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
Talarozole is a potent inhibitor of both CYP26A1 and CYP26B1, with IC50s of 5.4 and 0.46 nM, respectively.
Resorcinolnaphthalein is a specific angiotensin-converting enzyme 2 (ACE2) enhancer and activates ACE2 activity with an EC50 value of 19.5 μM. Resorcinolnaphthalein can be used for the investigation of hypertension and renal fibrosis[1].
RE-33 is an analgesic compound. RE-33 has blood brain barrier penetration ability[1].
MDL 27399 is an inhibitor of human neutrophil cathepsin G (Ki = 7 μM). MDL 27399 can be used for research of inflammatory diseases[1].
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity[1].
PGE-M is a metabolite of prostaglandin E2 (PEG2) as a biomarker of inflammation and cancer including advanced colorectal neoplasia, ovarian cancer, prostate cancer and so on. Urinary PGE-M is positively associated with obesity, smoking and lung metastases with breast cancer[1][2][3].
GSK-121 Trifluoroacetates a selective PAD4 inhibitor[1].
Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside is a orally active phenolic compound that can be isolated from the Geranium species. Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside has anti-inflammatory activities and has potential application in edema and aortic endothelium-dependent relaxation injury[1].
UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4[1][2].
DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
Telitacicept (RC18) is a fully human TACI-Fc fusion protein. Telitacicept is a dual B lymphocyte stimulator (BLyS)/APRIL (a proliferation-inducing ligand) inhibitor that effectively blocks proliferation of B lymphocytes. Telitacicept can be used in research of B-cell autoimmune disease[1].
Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50 = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively[1].
Calcipotriol Impurity C is the impurity of Calcipotriol, Calcipotriol is a ligand of VDR-like receptors.Target: VDR
Galactofucan (Fucogalactan) is a sulfated polysaccharide. Galactofucan can be extracted from brown seaweed Saccharina longicruris with anticoagulant, anti-tumor, anti-thrombosis, anti-inflammatory and antiviral properties. Galactofucan shows antiviral activities to HSV-1 and HSV-2 with IC50s of 0.76 and 1.34 µg/mL, respectively. Galactofucan can be used for the research of cancer and inflammation[1][2].
12-Hydroxy-2,3-dihydroeuparin (compound 7) is a natural product that can be isolated from the aerial parts of Ophryosporus axilliflorus. 12-Hydroxy-2,3-dihydroeuparin shows extremely anti-inflammatory activity[1].
Cardamonin (Cardamomin), a natural flavone isolated from Alpinia katsumadai Hayata, acts as an aryl hydrocarbon receptor (AhR) activator. Cardamonin alleviates inflammatory bowel disease by the inhibition of NLRP3 inflammasome activation via an AhR/Nrf2/NQO1 pathway[1].
Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research[1][2].
Cauloside C is a triterpene glycoside isolated from Caulophyllum robustum Max. Cauloside C exerts anti-inflammatory effects through the inhibition of expression of iNOS and proinflammatory cytokines[1].
Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody drug conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation[1].
Rimexolone (Org 6216) is a glucocorticoid steroid with anti-inflammatory activity. Rimexolone can be used as a 1% ophthalmic suspension for the management of ocular inflammation[1][2].
MrgprX2 antagonist-4 is an MrgprX2 antagonist extracted from patent US20210128561A1, compound B-51 E117. MrgprX2 antagonist-4 can be used for the research of inflammatory disorders of the skin[1].
Cimifugin is a major components of Yu-ping-feng-san, a Chinese medical formula that is used clinically for allergic diseases and characterized by reducing allergy relapse.
ABBV-712 is a selective inhibitor of Tyrosine kinase 2 (TYK2), with IC50 of 0.195 μM, that play important role in autoimmune diseases[1].
Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis[1].
Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. Fluorometholone acetate has anti-inflammatory effect and has the potential for external ocular inflammation research[1][2][3].
Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.Target: Histamine ReceptorAzatadine, a new antihistamine, was evaluated for its efficacy in 20 patients with chronic allergic rhinitis. Eighty percent of patients had symptomatic relief with a twice daily dosage of 2 mg. Sedation was volunteered as a side effect by six of the patients and was admitted by two further patients after specific questioning. A choice reaction time test gave slowing of motor function in these sedated patients. Four of the previously sedated patients experienced good symptomatic control with minimal sedation when the azatadine dose was reduced to 1 mg twice daily; slowing of motor function was not observed at this, the normal recommended dose.Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice.
SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research[1].
Guaiacol-13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].