Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
2-(Phosphonooxy)benzoic acid is a non-acetylated salicylic acid derivative which is used for treating inflammatory disease as well as in analgesic therapy[1].
17-Hydroxyneomatrine, extracted from Sophora flavescens, can well inhibit the growth of human cervical carcinoma Hela cells, has the wide-range antibacterial, anti-allergy, anti-tumor, anti-arrhythmia, swelling-subsiding diuresis, immunizing, and biological regulation functions[1].
Lys-Pro-Pro-Thr-Pro-Pro-Pro-Glu-Pro-Glu-Thr is a undecapeptide, corresponding to the carboxy terminus of simian virus 40 large T antigen. Lys-Pro-Pro-Thr-Pro-Pro-Pro-Glu-Pro-Glu-Thr can be targeted by antibodies secreted from three mouse hybridomas, designated KT1, KT3, and KT4, produced antibodies that immunoprecipitated large T antigen[1][2].
TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .IC50 Value: alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM [1]Target: integrinTR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 0.75 nM. TR14035 blocked binding of human alpha(4)beta(7)-expressing RPMI-8866 cells or murine mesenteric lymph node lymphocytes to MAdCAM-Ig with IC(50) values of 0.1 microM [2]. TR14035 blocked adhesion to HEVs [ED(50) of 0.01-0.1 mpk i.v.].TR-14035 was taken up by rat and human hepatocytes by an apparently single saturable mechanism with K(m) of 6.7 and 2.1 microM, respectively, and taurocholate and digoxin reduced this uptake [3].
Mesaconinean, an ingredient from Aconitum carmichaelii Debx., has cardiac effect[1].
N-Methylcalycinine is a nature product with AChE inhibitory activity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on[1].
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].
2-(N-Phthalimidoylmethylthio)acetic acid (MFA) is a hapten with a carboxyl group at the end of its spacer arm, suitable for reacting with free amine groups of proteins. 2-(N-Phthalimidoylmethylthio)acetic acid can be combined with carrier proteins and used in antigen design[1].
Taraxasterol is a pentacyclic triterpenoid isolated from Taraxacum officinale. Taraxasterol has a role as a metabolite and an anti-inflammatory agent[1].
PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively).
NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation[1].
Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[1] [2][3].
Wilforlide A is a natural product, separated from the ethanolic extract of tripterygium wilfordii. IC50 value:Target:In vitro:In vivo: Carrageenan-induced rat pedal swelling, tampon-induced rat granulation, and mice ear inhibition rate of swelling trail results show that high-dose wilforlide A has obvious anti-inflammatory effect, but has no significant immune suppressive activity [1].
Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide. Serum thymic factor induces hyperalgesia. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor has anti-diabetic, analgesic and anti-inflammatory effects[1][2][3].
SCD1-IN-1 is a SCD1 inhibitor (IC50: 5.8 nM). SCD1-IN-1 can be used in the research of dermatologic condition[1].
Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission[1].
IRAK4-IN-9 (compound 73) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-9 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer[1].
25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.
Tosufloxacin (tosylate hydrate) is a fluoroquinolone antibacterial agent. Tosufloxacin (tosylate hydrate) is effective against Gram-positive and Gram-negative aerobic bacteria, anaerobic bacteria and Chlamydia trachomatis. Tosufloxacin (tosylate hydrate) is also a bacterial Topo (DNA gyrase, topoisomerase)) inhibitor.
Risuteganib is an anti-integrin that downregulates oxidative stress and restores homeostasis, and targets three integrin receptors that are implicated in dry age-related macular degeneration (AMD) in order to restore homeostasis in the retina [1].
N-trans-Feruloyltyramine (N-feruloyltyramine), an alkaloid from Piper nigru, is an inhibitor of COX1 and COX2, with potential antioxidant properties. N-trans-Feruloyltyramine possesses anti-inflammatory activity[1].
Lidocaine Hcl salt, an amide local anesthetic, has anti-inflammatory properties in vitro and in vivo, possibly due to an attenuation of pro-inflammatory cytokines, intracellular adhesion molecule-1 (ICAM-1), and reduction of neutrophils influx.Target: Lidocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name xylocaine by Swedish chemist Nils Lofgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself.Lidocaine is approximately 95% metabolized (dealkylated) in the liver by CYP3A4 to the pharmacologically-active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half life than lidocaine but also is a less potent sodium channel blocker. The elimination half-life of lidocaine is approximately 90–120 minutes in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes).
Chitopentaose pentahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitopentaose pentahydrochloride is a substrate of gene encoding chitinase B (FjchiB)[1][2].
Emodin-6-O-β-D-glucoside (Glucoemodin) is an active compound from Reynoutria japonica. Emodin-6-O-β-D-glucoside shows potent anti-inflammatory and barrier protective effects. Emodin-6-O-β-D-glucoside can be used for the research of diabetic complications and atherosclerosis[1].
2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis), blocks BH4 synthesis and suppresses NO production[1].
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms[1]. PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].
L-Homocysteine, a homocysteine metabolite, is a homocysteine that has L configuration. L-Homocysteine induces upregulation of cathepsin V that mediates vascular endothelial inflammation in hyperhomocysteinaemia[1][2].
13-Hydroxygermacrone (compound 8) is a nature product that could be isolated form Curcuma zedoaria. 13-Hydroxygermacrone has anti-inflammatory effect[1].
Ergosterol peroxide glucoside is an Ergosterol derivative[1].