Hederagenin 28-O-beta-D-glucopyranosyl ester, a triterpenoid saponin isolated from Ilex cornuta, exhibits protective effects against H2O2-induced myocardial cell injury[1].
CCR1 inhibitor 19e is a novel potent, selective CCR1 antagonist with IC50 of 6.8 nM, inhibits CCR1chemotaxis in THP-1 cells with IC50 of 28 nM.
Clematichinenoside AR is a major active ingredient that could be extracted from the traditional Chinese herb Clematis chinensis and has potent pharmacological effects on various diseases, including atherosclerosis (AS)[1].
Bedinvetmab (ZTS-00508841) is a canine monoclonal antibody (mAb) targeting nerve growth factor (NGF). Bedinvetmab inhibits NGF interaction with tropomyosin receptor kinase A (trkA) and p75 neurotrophin receptor (p75NTR) receptors. Bedinvetmab can be used for the research of osteoarthritis pain in dogs[1][2].
ALR-6 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-6 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM and has no significant effect on direct inhibition of 5-LOX[1].
Tixocortol pivalate is a corticosteroid with some anti-inflammatory activity[1].
28-O-β-D-Glucopyranosyl pomolic acid is a urokinase plasminogen activator inhibitor with IC50 at 37.82 μM[1].
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants[1][2].
AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.
SM-324405 is a TLR7 agonist, with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively[1].
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1].
Stachyanthuside A is an ellagic acid glycoside isolated from the leaves of Diplopanax stachyanthus[1].
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a[1].
GSK-2250665A (Compound 13) is a selective Itk inhibitor with a pKi of 9.2.
Sirtuin modulator 3 (compound 129) is a N-phenyl benzamide derivative, acts as a sirtuin modulator[1].
Alginic acid is a natural polysaccharide, which has been widely concerned and applied due to its excellent water solubility, film formation, biodegradability and biocompatibility. Alginic acid induces oxidative stress-mediated hormone secretion disorder, apoptosis and autophagy in mouse granulosa cells and ovaries. Alginic acid has an inhibitory effect on histamine release. Anti-anaphylactic and anti-inflammatory properties[1][2][3].
BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription[1].
Poncirin is isolated from Poncirus trifoliata with anti-inflammory activites. Poncirin significantly reduces mechanical hyperalgesia and allodynia in Complete Freund’s Adjuvant (CFA)-induced inflammatory pain models[1].
Anti-inflammatory and analgesic agent
ATP ditromethamine (Adenosine 5'-triphosphate ditromethamine) is a central component of energy storage and metabolism in vivo. ATP ditromethamine provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP ditromethamine is an important endogenous signaling molecule in immunity and inflammation[1][2].
Rutin, a naturally occurring flavonoid glycoside, has antioxidant, anti-inflammatory, anti-allergic, anti-angiogenic and antiviral properties.
Tubeimoside III, a triterpenoid saponin isolated from a Chinese folk medicine"Tubeimu", shows anti-inflammatory, anti-tumor, anti-tumorigenic activities, and acute toxicity in vivo[1].
Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from unripe plantain banana. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models[1].
Stachyose hydrate act as a prebiotic to enhance the growth and activity of beneficial bacteria. Stachyose hydrate exhibit a hypoglycemic effect, and improve inflammation through modulating gut microbiota[1].
hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity[1].
Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated [1]. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom [2].
Carbetapentane citrate is a selective inhibitor of the cough, with mild atropine-like effect and local anesthesia effect.
Anakinra is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Anakinra is the first biological agent to block the pro-inflammatory effects[1][2].
(±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective[1][2][3][4][6].
Ro 19-1400 is a platelet-activating factor antagonist that directly inhibits immunoglobulin E-dependent mediator release[1].