Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma[1][2][3].
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites[1]. Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment[2].
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities[1][2].
Lexacalcitol (KH1060), a vitamin D analog, is potent regulators of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases[1][2].
Betamethasone-17-butyrate-21-propionate is a topical corticosteroid with potential in the treatment of inflammatory skin diseases.
AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM)[1]. AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma[2].
20-Hydroxy-leukotriene B4 is an endogenous metabolite present in Urine that can be used for the research of Sjogren Larsson Syndrome[1][2].
Pidotimod is an immunostimulant, a synthetic dipeptide with immunomodulatory properties, also able to increase the concentration of salivary IgA directed against bacteria.
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM)[1].
Antibacterial agent 54 (example 20) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Methyl 2-(2,4-dihydroxyphenyl)acetate, a phenolic ester, is isolated from Nigella damascena seeds with selective phytotoxic effects[1].
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research[1].
4(3H)-Quinazolinone is a building block in chemical synthesis. Biologically active nitrogen heterocyclic compounds. Possesses a wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancerous and analgesic activities[1][2].
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities[1][2][3].
Aselizumab (HuDreg-55) is an humanized IgG4 mAb against L-selectin. However, L-selectin (CD62L) is a cell adhesion molecule expressed on circulating neutrophils. It regulates migrating cells to chemotaxis towards the site of injury. Aselizumab may be account for a high rate of infections and leucopenia after truma[1][2].
SD-2590 hydrochloride is a potent MMP inhibitor with IC50 values of ﹤0.1, ﹤0.1, 0.18, and 1.7 nM for MMP2, MMP13, MMP9, and MMP8, respectively. SD-2590 hydrochloride inhibits dilation of the left ventricle in rats[1].
MART-1 (26-35) is amino acid residue 26 to 35 of MART-1 protein.
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects[1][2].
Lulizumab pegol (BMS-931699) is an anti-CD28 antibody antagonist. Lulizumab pegol effectively inhibits T-cell proliferation and it can be used for the reseach of kidney transplantation and autoimmunity disease[1].
MIF-IN-5 (compound 1d) is a potent and reversible macrophage migration inhibitory factor (MIF) competitive inhibitor with an IC50 of 4.8 μM and a Ki value of 3.3 μM, respectively[1].
RIPK-IN-4 is a potent and selective RIPK2 inhibitor with excellent oral bioavailability, and has an IC50 of 3 nM[1].
Stresscopin-related peptide (human) is a specific ligand for the type 2 CRH receptor. Stresscopin-related peptide (human) suppresses food intake, delayed gastric emptying and decreases heat-induced edema. Stresscopin-related peptide (human) maintains homeostasis after stress, and can be used in the research of stress-related diseases[1].
Dimethylamiloride hydrochloride is a Na+/H+ exchanger NHE inhibitor with Ki values of 0.02, 0.25, and 14 μM for NHE1, NHE2, and NHE3, respectively. Dimethylamiloride hydrochloride can be used for pain research[1].
Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.IC50 Value: 2.1 nM in pregnant C3H/HeN strain mice[5]Target: β2 receptorBudesonide/formoterol in a single inhaler for both maintenance and reliever therapy is now an established therapeutic option for management of inadequately controlled asthma[4].in vitro:. The long-acting β(2)-agonist formoterol and the glucocorticoid dexamethasone significantly reduced HRV-induced ERK phosphorylation, Fra-1, and MMP-9 expression in BEAS-2B cells[3].in vivo: compared the bronchodilatory effects of inhaled budesonide/formoterol (dose: 200 μg and 12 μg respectively) combination with budesonide (200 μg)/salbutamol (200 μg) administered by metered dose inhaler and spacer in children of 5-15 years with mild acute exacerbation of asthma [Modified Pulmonary Index Score (MPIS) between 6-8] in this double-blind, randomized controlled trial. The primary outcome was FEV1 (% predicted) in the two groups at 1, 5, 15, 30, 60 min after administration of the study drug[1]. Fifteen randomized, placebo-controlled clinical trials including COPD patients were evaluated: indacaterol 75 μg once daily (n = 2 studies), indacaterol 150 μg once daily (n = 5), indacaterol 300 μg once daily (n = 4), FOR/BUD 9/160 μg twice daily (n = 2), FOR/BUD 9/320 μg twice daily (n = 2), SAL/FP 50/500 μg twice daily (n = 4), and SAL/FP 50/250 μg twice daily (n = 1)[2].Clinical trial: Effects of Mometasone Furoate/Formoterol Combination Versus Mometasone Furoate Alone in Persistent Asthmatics (Study P04073) . Phage3
MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders[1].
Cholesterylamine is a cationic lipid. Cholesterylamine can be added to the PLGA to prepare PLGA particle having surface charge. Cholesterylamine can be used for drug delivery. Cholesterylamine can be used for autoimmune diseases and allergy research[1].
GSK217 (GSK-217) is a potent, highly selective BET BD2 inhibitor with pIC50 of 7.5 (BRD4 BD2), 300-fold selectivity over BRD4 BD1.
Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response[1][2].